1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: Lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity

被引：61

作者：

Hale, JJ ^{[1
]}

Budhu, RJ

Holson, EB

Finke, PE

Oates, B

Mills, SG

MacCoss, M

Gould, SL

DeMartino, JA

Springer, MS

Siciliano, S

Malkowitz, L

Schleif, WA

Hazuda, D

Miller, M

Kessler, J

Danzeisen, R

Holmes, K

Lineberger, J

Carella, A

Carver, G

Emini, E

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(01)00545-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Investigations of the structure-activity relationships of 1,3,4-trisubstituted pyrrolidine human CCR5 receptor antagonists afforded orally bioavailable compounds with the ability to inhibit HIV replication in vitro. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2741 / 2745

页数：5

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