1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: Discovery of the pyrrolidine scaffold and determination of its stereochemical requirements

被引：55

作者：

Hale, JJ ^{[1
]}

Budhu, RJ

Mills, SG

MacCoss, M

Malkowitz, L

Siciliano, S

Gould, SL

DeMartino, JA

Springer, MS

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Immunol Res, Rahway, NJ 07065 USA

来源：

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

关键词：

D O I：

10.1016/S0960-894X(01)00232-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [I-125]-MIP-1 alpha from the CCR5 receptor expressed on Chinese hamster ovary (CHO) cell membranes. CCR5 activity was found to be dependent on the regiochemistry and the absolute stereochemistry of the pyrrolidine. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：1437 / 1440

页数：4

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