Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure-activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl)butanes
被引:88
作者:
Dorn, CP
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Dorn, CP
Finke, PE
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Finke, PE
Oates, B
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Oates, B
Budhu, RJ
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Budhu, RJ
Mills, SG
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Mills, SG
MacCoss, M
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
MacCoss, M
Malkowitz, L
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Malkowitz, L
Springer, MS
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Springer, MS
Daugherty, BL
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Daugherty, BL
Gould, SL
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Gould, SL
DeMartino, JA
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
DeMartino, JA
Siciliano, SJ
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Siciliano, SJ
Carella, A
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Carella, A
Carver, G
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Carver, G
Holmes, K
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Holmes, K
Danzeisen, R
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Danzeisen, R
Hazuda, D
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Hazuda, D
Kessler, J
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Kessler, J
Lineberger, J
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Lineberger, J
Miller, M
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Miller, M
Schleif, WA
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Schleif, WA
Emini, EA
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机构:Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
Emini, EA
机构:
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Immunol Res, Rahway, NJ 07065 USA
[3] Merck Res Labs, Dept Antiviral Res, W Point, PA 19486 USA
Screening of the Merck sample collection for compounds with CCR5 receptor binding afforded (2S)-2-(3,4-dichlorophenyl)- 1-[N-(methyl)-N-(phenylsulfonyl)amino]-4,4'-piperidin-1'-yl)]butane S-oxide (4) as a potent lead structure having an IC50 binding affinity of 35 nM. Herein, we describe the discovery of this lead structure and our initial structure-activity relationship studies directed toward the requirement for and optimization of the 1-amino fragment. (C) 2001 Published by Elsevier Science Ltd.