1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: Polar functionality and its effect on anti-HIV-1 activity

被引:26
作者
Hale, JJ [1 ]
Budhu, RJ
Mills, SG
MacCoss, M
Gould, SL
DeMartino, JA
Springer, MS
Siciliano, SJ
Malkowitz, L
Schleif, WA
Hazuda, D
Miller, M
Kessler, J
Danzeisen, R
Holmes, K
Lineberger, J
Carella, A
Carver, G
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
关键词
D O I
10.1016/S0960-894X(02)00605-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Incorporation of acidic functional groups into a lead CCR5 antagonist identified from a targeted combinatorial library resulted in compounds with enhanced anti-HIV-1 activity and attenuated L-type calcium channel affinity. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2997 / 3000
页数:4
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