Combinatorial synthesis of CCR5 antagonists

被引：41

作者：

Willoughby, CA ^{[1
]}

Berk, SC

Rosauer, KG

Degrado, S

Chapman, KT

Gould, SL

Springer, MS

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, West Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(01)00652-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Herein we report the preparation of a combinatorial library of compounds with potent CCR5 binding affinity. The library design was aided by SAR generated in a traditional medicinal chemistry effort. Compounds with novel combinations of subunits were discovered that have high binding affinity for the CCR5 receptor. A potent CCR5 antagonist from the library, compound 11 was found to have moderate anti-HIV-1 activity. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：3137 / 3141

页数：5

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