SCOPUS 정보 검색 플랫폼

Journal of the American Chemical Society

Volumn 119, Issue 16, 1997, Pages 3696-3708

Solution phase combinatorial chemistry. Discovery of novel polyazapyridinophanes with potent antibacterial activity by a solution phase simultaneous addition of functionalities approach

(10) An, Haoyun a Cummins, Lendell L a Griffey, Richard H a Bharadwaj, Ramesh a Haly, Becky D a Fraser, Allister S a Wilson Lingardo, Laura a Risen, Lisa M a Wyatt, Jacqueline R a Cook, P Dan a

a ISIS PHARMACEUTICALS (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMINE; ANTIINFECTIVE AGENT; MACROCYCLIC COMPOUND; PYRIDINE DERIVATIVE;

ARTICLE; DRUG SYNTHESIS; IN VITRO STUDY; MASS SPECTROMETRY; METHODOLOGY; REACTION ANALYSIS; ZONE ELECTROPHORESIS;

EID: 0030959257 PISSN: 00027863 EISSN: None Source Type: Journal
DOI: 10.1021/ja964153r Document Type: Article

Times cited : (78)

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76
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- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1992) J, Am. Chem. Soc. , vol.114 , pp. 10997
- Bunin, B.A.¹ Ellman, J.A.²

77
- 0028278170
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1994) Proc. Natl. Acad. Sci. U.S.A. , vol.91 , pp. 4708
- Bunin, B.A.¹ Plunkett, M.J.² Ellman, J.A.³

78
- 0028928237
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1995) J. Am. Chem. Soc. , vol.117 , pp. 3306
- Plunkett, M.J.¹ Ellman, J.A.²

79
- 0027202613
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1993) Proc. Natl. Acad. Sci. U.S.A. , vol.90 , pp. 6909
- DeWitt, S.H.¹ Kiely, J.S.² Stankovic, C.J.³ Schroeder, M.C.⁴ Reynolds Cody, D.M.⁵ Pavia, M.R.⁶

80
- 0030034999
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 937
- Dressman, B.A.¹ Spangle, L.A.² Kaldor, S.W.³

81
- 0030064961
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) J. Am. Chem. Soc. , vol.118 , pp. 253
- Ruhland, B.¹ Bhandari, A.² Gordon, E.M.³ Gallop, M.A.⁴

82
- 0028833961
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1995) Bioorg. Med. Chem. Lett. , vol.5 , pp. 47
- Gordon, D.W.¹ Steele, J.²

83
- 0030038838
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) J. Org. Chem. , vol.61 , pp. 924
- Gordeev, M.F.¹ Patel, D.V.² Gordon, E.M.³

84
- 0030200397
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 4643
- Gordeev, M.F.¹ Patel, D.V.² Wu, J.³ Gordon, E.M.⁴

85
- 0141856793
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedon Lett. , vol.37 , pp. 4815
- MacDonald, A.A.¹ DeWitt, S.H.² Hogan, E.M.³ Ramage, R.⁴

86
- 0030600160
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 4439
- Buckman, B.O.¹ Mohan, R.²

87
- 0030576328
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Bioorg. Med. Chem. Lett. , vol.6 , pp. 1483
- Smith, A.L.¹ Thomson, C.G.² Leeson, P.D.³

88
- 0030575349
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am.
- (1996) Tetrahedron Lett. , vol.37 , pp. 4865
- Hutchins, S.M.¹ Chapman, K.T.²

89
- 0029940759
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 2943
- Mjalli, A.M.M.¹ Sarshar, S.² Baiga, T.J.³

90
- 0030575421
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 4869
- Hutchins, S.M.¹ Chapman, K.T.²

91
- 0030575422
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 4887
- Phillips, G.B.¹ Wei, G.P.²

92
- 85047674714
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1995) Tetrahedron Lett. , vol.37 , pp. 4923
- Dankwardt, S.M.¹ Newman, S.R.² Krstenansky, J.L.³

93
- 0030581332
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 5839
- Kowalski, J.¹ Lipton, M.A.²

94
- 0030593622
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 6073
- Cao, X.¹ Mjalli, A.M.M.²

95
- 0030605892
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 5457
- Zhang, C.¹ Mjalli, A.M.M.²

96
- 0029883219
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) J. Org. Chem. , vol.61 , pp. 4494
- Koh, J.S.¹ Ellman, J.A.²

97
- 0030570866
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 5633
- Mayer, J.P.¹ Bankaitis-Davis, D.² Zhang, J.³ Beaton, G.⁴ Bjergarde, K.⁵ Andersen, C.M.⁶ Goodman, B.A.⁷ Herrera, C.J.⁸

98
- 0030586143
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 5041
- Yang, L.¹ Guo, L.²

99
- 0029740469
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) J. Am. Chem. Soc. , vol.118 , pp. 7430
- Norman, T.C.¹ Gray, N.S.² Koh, J.T.³ Schultz, P.G.⁴

100
- 0029681546
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Tetrahedron Lett. , vol.37 , pp. 5277
- Kolodziej, S.A.¹ Hamper, B.C.²

101
- 0030182486
- For recent combinatorial libraries based on known pharmacophores, see the following. Benzodiazepines: Bunin, B. A.; Ellman, J. A. J, Am. Chem. Soc. 1992, 114, 10997. Bunin, B. A.; Plunkett, M. J.; Ellman, J. A. Proc. Natl. Acad. Sci. U.S.A. 1994, 91, 4708. Plunkett, M. J.; Ellman, J. A. J. Am. Chem. Soc. 1995, 117, 3306. Hydantoins: DeWitt, S. H.; Kiely, J. S.; Stankovic, C. J.; Schroeder, M. C.; Reynolds Cody, D. M.; Pavia, M. R. Proc. Natl. Acad. Sci. U.S.A. 1993, 90, 6909. Dressman, B. A.; Spangle, L. A.; Kaldor, S. W. Tetrahedron Lett. 1996, 37, 937. β-Lactams: Ruhland, B.; Bhandari, A.; Gordon, E. M.; Gallop, M. A. J. Am. Chem. Soc. 1996, 118, 253. Piperazineidones: Gordon, D. W.; Steele, J. Bioorg. Med. Chem. Lett. 1995, 5, 47. 1,4-Dihydropyridines: Gordeev, M. F.; Patel, D. V.; Gordon, E. M. J. Org. Chem. 1996, 61, 924. Pyridines and pyrido-[2,3]pyrimidines: Gordeev, M. F.; Patel, D. V.; Wu, J.; Gordon, E. M. Tetrahedron Lett. 1996, 37, 4643. Quinolines: MacDonald, A. A.; DeWitt, S. H.; Hogan, E. M.; Ramage, R. Tetrahedon Lett. 1996, 37, 4815. Buckman, B. O.; Mohan, R. Tetrahedron Lett. 1996, 37, 4439. Smith, A. L.; Thomson, C. G.; Leeson, P. D. Bioorg. Med. Chem. Lett. 1996, 6, 1483. Tetrahydroisoquinolines and tetrahydroimidazopyridines: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4865. Pyrroles: Mjalli, A. M. M.; Sarshar, S.; Baiga, T. J. Tetrahedron Lett. 1996, 37, 2943. Indoles: Hutchins, S. M.; Chapman, K. T. Tetrahedron Lett. 1996, 37, 4869. Benzimidazoles: Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1996, 37, 4887. Piperazines: Dankwardt, S. M.; Newman, S. R.; Krstenansky, J. L. Tetrahedron Lett. 1995, 37, 4923. Kowalski, J.; Lipton, M. A. Tetrahedron Lett. 1996, 37, 5839. Phosphonates: Cao, X.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 6073. Zhang, C.; Mjalli, A. M. M. Tetrahedron Lett. 1996, 37, 5457. Tropanes: Koh, J. S.; Ellman, J. A. J. Org. Chem. 1996, 61. 4494. Tetrahydro-β-carbolines: Mayer, J. P.; Bankaitis-Davis, D.; Zhang, J.; Beaton, G.; Bjergarde, K.; Andersen, C. M.; Goodman, B. A.; Herrera, C. J. Tetrahedron Lett. 1996, 37, 5633. Yang, L.; Guo, L. Tetrahedron Lett. 1996, 37, 5041. Purines: Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz. P. G. J. Am. Chem. Soc. 1996, 118, 7430. Dihydropyrimidinediones: Kolodziej, S. A.; Hamper. B. C. Tetrahedron Lett. 1996, 37, 5277. Rauwolfina alkaloids: Atuegbu, A.; Maclean, D.; Nguyen, C.; Gordon, E. M.; Jacobs, J, W. Bioorg. Med. Chem. 1996,4, 1097. Miconazole: Tortolani, D. R.; Biller, S. A. Tetrahedron Lett. 1996, 37, 5687.
- (1996) Bioorg. Med. Chem. , vol.4 , pp. 1097
- Atuegbu, A.¹ Maclean, D.² Nguyen, C.³ Gordon, E.M.⁴ Jacobs, J.W.⁵

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- For example, consider a polyazaphane scaffold with four sites to combinatorialize and with one "fixed" or selectively protected site. In the simplest situation (one step for deprotection), 48 reactions are required to completely deconvolute (find the single active compound) for a fix-last process. This consists of (1) a simultaneous addition reaction step using all functional groups, (2) a deprotecting step, (3) a division of the material into 10 pools (assuming 10 functionalities), and (4) reaction of each pool with an individual functionality at the fixed position (the pools are all screened). To do this for four combinatorial sites requires 48 reactions (4 × 12) assuming the scaffold is available as an orthogonally protected species. If the same scaffold is deconvoluted by a fix-first process, 110 reactions are required. This requires (1) a deprotection step of the orthogonally protected scaffold (note to start this approach requires the synthesis of a fully orthogonally protected scaffold), (2) separation into 10 pools, (3) reaction of each pool with each functionality, and (4) repetition of the entire process three times: thus, in total. (4 × 11) reactions (first round) + (3 × 11) reactions (second round) + (2 × 11) reactions (third round) + ( 1 × 11) reactions (fourth round) =110 reactions to completely deconvolute by a fix-first process. The number of steps in the fix-first process increases as the number of sites increases relative to the fix-last process (e.g., for 10 functionalities and five sites: fix-first for first round = 55 reactions vs 12 for fix-last, and to completely deconvolute is 165 reactions r.v 60 reactions, and with six sites the first round is 66 vs 12 reactions, and 231 vs 72 reaction are needed to completely deconvolute). Possibly more important is the likelihood that a high percentage of first-round libraries will not be active in a particular assay, and thus subsequent deconvolution is not required, a potential saving of many reaction steps. In the case of fix-last, a completely orthogonally protected scaffold is not initially required to obtain first-round libraries. In the case of a fix-first process, considerable protection chemistry is required to start the process since completely orthogonally protected scaffold is required and will be of little value if activity is not found in the first round. Furthermore, orthogonally protecting more than three sites can be synthetically challenging.

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- Hodgkinson, L.C.¹ Sutherland, I.O.²

113
- 0029119899
- Fukuyama, T.; Jow, C-K.; Cheung, M. Tetrahedron Lett. 1995, 36, 6373.
- (1995) Tetrahedron Lett. , vol.36 , pp. 6373
- Fukuyama, T.¹ Jow, C.-K.² Cheung, M.³

114
- 1842272894
- Unpublished results
- Kung, P. P.; Fraser, A. S.; Guinosso, C. J.; Bharadwaj, R.; Cook, P. D. Unpublished results.
- Kung, P.P.¹ Fraser, A.S.² Guinosso, C.J.³ Bharadwaj, R.⁴ Cook, P.D.⁵

115
- 0029044308
- O'Sullivan, M. C; Dalrymple, D. M. Tetrahedron Lett. 1995, 36, 3451.
- (1995) Tetrahedron Lett. , vol.36 , pp. 3451
- O'Sullivan, M.C.¹ Dalrymple, D.M.²

116
- 1842270954
- note
- The column loaded with a crude library was eluted with a less polar solvent to remove the excess benzylic bromides and then was eluted with more polar solvents to completely remove the library. All fractions containing library compounds were collected. The preparative thin layer chromatography (PLC) loaded with crude library was developed by selected solvents. The library band, which was generally wider than those of single compounds, was collected to provide pure library without electrophiles and other impurities.

117
- 1842391401
- note
- 1H NMR spectra of libraries show the correct ratio of certain protons. The ESI mass spectra show the peaks ranging from the smallest molecular weight to the largest molecular weight in libraries.

118
- 1842319945
- note
- Our current requirement for the libraries is that the molar differences of theoretical amounts and the detected amounts of all compounds in one library are within 20%. The active compounds within this deviation would not be missed using our antibacterial assays.

119
- 1842400213
- note
- The theoretical yield was calculated according to the average molecular weight. The yield was obtained by comparing the amount of isolated library with the theoretical yield.

120
- 1842303753
- note
- Library 7 has the following 49 theoretically different molecular weights: 518, 532, 536, 543, 544, 546, 550, 552, 554, 557, 558, 561, 562, 563, 566, 568, 569, 570, 576, 577, 578, 581, 586, 588, 589, 590, 594, 597, 600, 601, 602, 604, 608, 610, 611, 612, 614, 620, 621, 622, 623, 631, 634, 641, 644, 654, 655, 664, 676.

121
- 1842267053
- MCCLS Document M7-A3, Villanova. PA
- National Committee for Clinical Laboratory Standards. Methods for Dilution Antimicrobial Susceptibility Tests for Bacterial that Grow Aerobically, 1993; MCCLS Document M7-A3, Vol. 13, Villanova. PA.
- (1993) Methods for Dilution Antimicrobial Susceptibility Tests for Bacterial That Grow Aerobically , vol.13

122
- 0024690869
- Sampson, B. A.; Misra, R.; Benson, S. A. Genetics 1989,122,491.
- (1989) Genetics , vol.122 , pp. 491
- Sampson, B.A.¹ Misra, R.² Benson, S.A.³

* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.