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Recent Developments in HIV Protease Inhibitor Research
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(a) Chrusciel, R. A.; Homines, K. R. Recent Developments in HIV Protease Inhibitor Research. Expert Opin. Ther. Pat. 1997, 7, 111-121.
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Viral Dynamics of HIV: Implications for Drug Development and Therapeutic Strategies
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The End of AIDS
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Leland, J.1
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HFV-1 Protease Inhibitors: A Review for Clinicians
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(a) Deeks, S. G.; Smith, M.; Holodniy, M.; Kahn, J. O. HFV-1 Protease Inhibitors: A Review for Clinicians. J. Am. Med. Assoc. 1997, 277, 145-153.
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Current Knowledge and Future Prospects for the Use of HIV Protease Inhibitors
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Obstacles to Drug Development from Peptide Leads
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(a) Plattner, J. J.; Norbeck, D. W. Chapter 5. Obstacles to Drug Development from Peptide Leads. In Drug Discovery Technologies; Clark, C. R., Moos, W. H., Eds.; Ellis Horwood: Chichester, England, 1990; pp 92-126. (b) Barry, M.; Gibbons, S.; Back, D.; Mulcahy, F. Protease Inhibitors in Patients with HIV Disease. Clin Pharmacokinet. 1997, 32, 194-209.
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Protease Inhibitors and Nucleoside Combinations
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(a) Mascolini, M. Protease Inhibitors and Nucleoside Combinations. J. Int. Assoc. Physicians AIDS Care 1996, 4, 23-33.
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New Aids Treatment Raises Tough Question of Who Will Get It
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Waldholz, M.1
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Discovery and Optimization of Nonpeptide HIV-1 Protease Inhibitors
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Tummino, P. J.; Vara Prasad, J. V. N.; Ferguson, D.; Nouhan, C.; Graham, N.; Domagala, J. M.; Ellsworth, E.; Gajda, C.; Hagen, S. E.; Lunney, E. A.; Para, K. S.; Tait, B. D.; Pavlovsky, A.; Erickson, J. W.; Gracheck, S.; McQuade, T. J.; Hupe, D. J. Discovery and Optimization of Nonpeptide HIV-1 Protease Inhibitors. Bioorg. Med. Chem. 1996, 4, 1401-1404.
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Tummino, P.J.1
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Domagala, J.M.6
Ellsworth, E.7
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0029586468
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4-Hydroxypyrones and Related Templates as Nonpeptidic HIV Protease Inhibitors
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(a) Romines, K. R.; Chrusciel, R. A. 4-Hydroxypyrones and Related Templates as Nonpeptidic HIV Protease Inhibitors. Curr. Med. Chem. 1995, 2, 825-838.
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Romines, K.R.1
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0029909674
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Structure-Based Design of HIV Protease Inhibitors: Sulfonamide-Containing 5,6-Dihydro-4-hydroxy-2-pyrones as Non-Peptidic Inhibitors
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(b) Thaisrivongs, S.; Skulnik, H. I.; Turner, S. R.; Strohbach, J. W.; Tommasi, R. A.; Johnson, P. D.; Aristoff, P. A.; Judge, T. M.; Gammill, R. B.; Morris, J. K.; Romines, K R.; Ch'rusciel, R. A.; Hinshaw, R. R.; Chong, K.-T.; Tarpley, W. G.; Poppe, S. M.; Slade, D. E.; Lynn, J.- C.; Horng, M.-M.; Tomich, P. K.; Seest, E. P.; Dolak, L. A.; Howe, W. J.; Howard, G. M.; Schwende, F. J.; Toth, L. N.; Padbury, G. E.; Wilson, G. J.; Shiou, L.; Zipp, G. L.; Wilkinson, K. F.; Rush, B. D.; Ruwart, M. J.; Koeplinger, K. A.; Zhao, Z.; Cole, S.; Zaya, R. M.; Kakuk, T. J.; Janakiraman, M. N.; Watenpaugh, K. D. Structure-Based Design of HIV Protease Inhibitors: Sulfonamide-Containing 5,6-Dihydro-4-hydroxy-2-pyrones as Non-Peptidic Inhibitors. J. Med. Chem. 1996, 39, 4349-4353.
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Thaisrivongs, S.1
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Johnson, P.D.6
Aristoff, P.A.7
Judge, T.M.8
Gammill, R.B.9
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Ch'Rusciel, R.A.12
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Chong, K.-T.14
Tarpley, W.G.15
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Slade, D.E.17
Lynn, J.C.18
Horng, M.-M.19
Tomich, P.K.20
Seest, E.P.21
Dolak, L.A.22
Howe, W.J.23
Howard, G.M.24
Schwende, F.J.25
Toth, L.N.26
Padbury, G.E.27
Wilson, G.J.28
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Zipp, G.L.30
Wilkinson, K.F.31
Rush, B.D.32
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Janakiraman, M.N.39
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0028094959
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Novel Series of Achiral, Low Molecular Weight, and Potent HIV-1 Protease Inhibitors
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Vara Prasad, J. V. N.; Para, K. S.; Lunney, E. A.; Ortwine, D. F.; Dunbar, J. B.; Ferguson, D.; Tummino, P. J.; Hupe, D.; Tait, B. D.; Domagala, J. M.; Humblet, C.; Bhat, T. N.; Liu, B.; Guerin, D. M. A.; Baldwin, E. T.; Erickson, Sawyer, T. K. Novel Series of Achiral, Low Molecular Weight, and Potent HIV-1 Protease Inhibitors. J. Am. Chem. Soc. 1994,116, 6989-6990.
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Vara Prasad, J.V.N.1
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Ferguson, D.6
Tummino, P.J.7
Hupe, D.8
Tait, B.D.9
Domagala, J.M.10
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4-Hydroxy-5,6dihydropyrones. 2. Potent Non-Peptide Inhibitors of HIV Protease
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Tait, B. D.; Domagala, J. M.; Ellsworth, E. L.; Gajda, C.; Hagen, S. E.; Hamilton, H.; Vara Prasad, J. V. N.; Ferguson, D.; Graham, N.; Hupe, D.; Nouhan, C.; Tummino, P. J.; Humblet, C.; Lunney, E. A.; Pavlovsky, A.; Rubin, R. J.; Baldwin, E. T.; Bhat, T. N.; Erickson, J. W.; Gulnik, S.; Liu, B. 4-Hydroxy-5,6dihydropyrones. 2. Potent Non-Peptide Inhibitors of HIV Protease. J. Med. Chem. 1997, 40, 3781-3792.
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A Facile Synthesis of Unsymmetrical Thiosulfonates via Sulfonylation of Mercaptans
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Ranasinghe, M. G.; Fuchs, P. L. A Facile Synthesis of Unsymmetrical Thiosulfonates via Sulfonylation of Mercaptans. Synth. Commun. 1988,18, 227-232.
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The Conversion of Phenols to Thiophenols via Dialkylthiocarbamates
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Competitive Inhibition of HIV-1 Protease by Biphenyl Carboxylic Acids
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Experimental conditions for the enzyme assay at pH 4.7: Tummino, P. J.; Ferguson, D.; Jacobs, C. M.; Tait, B. D.; Hupe, L.; Lunney, E.; Hupe, D. Competitive Inhibition of HIV-1 Protease by Biphenyl Carboxylic Acids. Arch. Biochem. Biophys. 1995,316,523-528. This procedure was modified slightly when run at pH 6.2: the buffer was changed to 1.0 mM dithiothreitol, 80 mM MES, 160 mM NaCl, 1.0 mM EDTA, and 0.1% polyethylene glycol (MW 8000). The final concentration of HIV protease used was 1.5 nM.
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Tummino, P.J.1
Ferguson, D.2
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Hupe, L.5
Lunney, E.6
Hupe, D.7
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Thiazolobenzimidazole: Biological and Biochemical Anti-retroviral Activity of a New Nonnucleoside Reverse Transcriptase Inhibitor
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Buckheit, R. W., Jr.; Hollingshead, M. G.; Germany-Decker, J.; White, L.; McMahon, J. B.; Alien, L. B.; Ross, L. J.; Decker, W. D.; Westbrook, L.; Shannon, W. M.; Weislow, O.; Bader, J. P.; Boyd, M. R. Thiazolobenzimidazole: Biological and Biochemical Anti-retroviral Activity of a New Nonnucleoside Reverse Transcriptase Inhibitor. Antiviral Res. 1993, 21, 247-265.
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