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1
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0028341682
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2-Azetidinones as inhibitors of cholesterol absorption
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Burnett, D. A.; Caplen, M. A.; Davis, H. R., Jr.; Burner, R. E.; Clader, J. W. 2-Azetidinones as inhibitors of cholesterol absorption. J. Med. Chem. 1994, 37, 1733-1736. For related recent work in this area, see: Clader, J. W.; Burnett, D. A.; Caplen, M. A.; Domalski, M. S.; Dugar, S.; Vaccaro, W.; Sher, R.; Browne, M. E.; Zhao, H.; Burner, R. E.; Salisbury, B.; Davis, H. R., Jr. 2-Azetidinone cholesterol absorption inhibitors: Structure-activity relationships on the heterocyclic nucleus. J. Med. Chem. 1996, 39, 3684-3693. Rosenblum, S. B.; Huynh, T.; Afonso, A.; Davis, H. R., Jr.; Yumibe, N.; Clader, J. W.; Burnett, D. A. Discovery of SCH 58235: A designed potent orally active inhibitor of cholesterol absorption. J. Med. Chem. 1998, submitted.
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J. Med. Chem.
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Burnett, D.A.1
Caplen, M.A.2
Davis Jr., H.R.3
Burner, R.E.4
Clader, J.W.5
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2
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9544237127
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2-Azetidinone cholesterol absorption inhibitors: Structure-activity relationships on the heterocyclic nucleus
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Burnett, D. A.; Caplen, M. A.; Davis, H. R., Jr.; Burner, R. E.; Clader, J. W. 2-Azetidinones as inhibitors of cholesterol absorption. J. Med. Chem. 1994, 37, 1733-1736. For related recent work in this area, see: Clader, J. W.; Burnett, D. A.; Caplen, M. A.; Domalski, M. S.; Dugar, S.; Vaccaro, W.; Sher, R.; Browne, M. E.; Zhao, H.; Burner, R. E.; Salisbury, B.; Davis, H. R., Jr. 2-Azetidinone cholesterol absorption inhibitors: Structure-activity relationships on the heterocyclic nucleus. J. Med. Chem. 1996, 39, 3684-3693. Rosenblum, S. B.; Huynh, T.; Afonso, A.; Davis, H. R., Jr.; Yumibe, N.; Clader, J. W.; Burnett, D. A. Discovery of SCH 58235: A designed potent orally active inhibitor of cholesterol absorption. J. Med. Chem. 1998, submitted.
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J. Med. Chem.
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Clader, J.W.1
Burnett, D.A.2
Caplen, M.A.3
Domalski, M.S.4
Dugar, S.5
Vaccaro, W.6
Sher, R.7
Browne, M.E.8
Zhao, H.9
Burner, R.E.10
Salisbury, B.11
Davis Jr., H.R.12
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3
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0028341682
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Discovery of SCH 58235: A designed potent orally active inhibitor of cholesterol absorption
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submitted
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Burnett, D. A.; Caplen, M. A.; Davis, H. R., Jr.; Burner, R. E.; Clader, J. W. 2-Azetidinones as inhibitors of cholesterol absorption. J. Med. Chem. 1994, 37, 1733-1736. For related recent work in this area, see: Clader, J. W.; Burnett, D. A.; Caplen, M. A.; Domalski, M. S.; Dugar, S.; Vaccaro, W.; Sher, R.; Browne, M. E.; Zhao, H.; Burner, R. E.; Salisbury, B.; Davis, H. R., Jr. 2-Azetidinone cholesterol absorption inhibitors: Structure-activity relationships on the heterocyclic nucleus. J. Med. Chem. 1996, 39, 3684-3693. Rosenblum, S. B.; Huynh, T.; Afonso, A.; Davis, H. R., Jr.; Yumibe, N.; Clader, J. W.; Burnett, D. A. Discovery of SCH 58235: A designed potent orally active inhibitor of cholesterol absorption. J. Med. Chem. 1998, submitted.
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Rosenblum, S.B.1
Huynh, T.2
Afonso, A.3
Davis Jr., H.R.4
Yumibe, N.5
Clader, J.W.6
Burnett, D.A.7
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4
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0028912542
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Hypercholesterolemic activity of a novel inhibitor of cholesterol absorption, SCH 48461
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1 had demonstrated only weak ACAT activity for a series of structurally related azetidinones. Therefore it is highly unlikely that the weak ACAT activity that these compounds may have would account for the potent CAI activity observed.
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Atherosclerosis
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Salisbury, B.G.1
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Clemmons, A.L.7
Compton, D.S.8
Hoos, L.M.9
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Schnitzer-Polokoff, R.11
Smith, A.A.12
Weig, B.C.13
Zilli, D.L.14
Clader, J.W.15
Sybertz, E.J.16
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5
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0003250723
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The clinical development of a novel cholesterol absorption inhibitor
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Bergman, M.; Morales, H.; Meilars, L.; Kosoglou, T.; Burner, R.; Davis, H. R.; Sybertz, E. J.; Pollare, T. The clinical development of a novel cholesterol absorption inhibitor. 12th International Symposium on Drugs Affecting Lipid Metabolism, 1995.
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Bergman, M.1
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Kosoglou, T.4
Burner, R.5
Davis, H.R.6
Sybertz, E.J.7
Pollare, T.8
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6
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0030594964
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Stereoselective synthesis and biological activity of cis azetidinones as cholesterol absorption inhibitors
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McKittrick, B. A.; Ma, K.; Dugar, S.; Clader, J. W.; Davis, H., Jr.; Czarniecki, M.; McPhail, A. T. Stereoselective synthesis and biological activity of cis azetidinones as cholesterol absorption inhibitors. Bioorg. Med. Chem. Lett. 1996, 6, 1947-1950.
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McKittrick, B.A.1
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Dugar, S.3
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Davis Jr., H.5
Czarniecki, M.6
McPhail, A.T.7
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7
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15644374490
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Rosenblum, S. B.; Huynh, T.; Davis, H.; Yumibe, N.; Clader, J.; Afonso, A.; Burnett, D. B. International Symposium on Drugs Affecting Lipid Metabolism, 1995.
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Rosenblum, S.B.1
Huynh, T.2
Davis, H.3
Yumibe, N.4
Clader, J.5
Afonso, A.6
Burnett, D.B.7
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8
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0030848734
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In vivo metabolism-based discovery of a potent cholesterol absorption inhibitor, SCH 58235, in the rat and Rhesus monkey through the identification of the active metabolites of SCH 48461
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Van Heek, M.; France, C. F.; Compton, D. S.; McLeod, R. L.; Yumibe, N. P.; Alton, K. B.; Sybertz, E. J.; Davis, H. R In vivo metabolism-based discovery of a potent cholesterol absorption inhibitor, SCH 58235, in the rat and Rhesus monkey through the identification of the active metabolites of SCH 48461. JPET 1997, 283, 157-163.
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0029975253
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Metabolism and structure activity data based drug design: Discovery of (-) SCH 53079 an analogue of the potent cholesterol absorption inhibitor (-) SCH 48461
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Dugar, S.; Yumibe, N.; Clader, J. W.; Vizziano, M.; Huie, K.; Van Heek, M.; Compton, D. S.; Davis, H. R., Jr. Metabolism and structure activity data based drug design: Discovery of (-) SCH 53079 an analogue of the potent cholesterol absorption inhibitor (-) SCH 48461. Bioorg. Med. Chem. Lett. 1996, 6, 2069-2073
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New procedure for the direct generation of titanium enolates. Diastereoselective bond constructions with representative electrophiles
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Sulfonic acidsodium iodide system as an efficient reagent for the reduction of sulfoxides
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Chelation control in metal-assisted aldol reactions of α-halogenated imide enolates leading to predominately anti stereoselectivity. An example of a stereocontrolled Darzens reaction
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Pridgen, L. N.; Abdel-Magid, A.; Lantos, I.; Shilcrat, S.; Eggleston, D. Chelation control in metal-assisted aldol reactions of α-halogenated imide enolates leading to predominately anti stereoselectivity. An example of a stereocontrolled Darzens reaction. J. Org. Chem. 1993, 55, 5107.
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