1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: Modifications of the arylpropylpiperidine side chains

被引：51

作者：

Lynch, CL

Willoughby, CA

Hale, JJ

Holson, EJ

Budhu, RJ

Gentry, AL

Rosauer, KG

Caldwell, CG

Chen, P

Mills, SG

MacCoss, M

Berk, S

Chen, L

Chapman, KT

Malkowitz, L

Springer, MS

Gould, SL

DeMartino, JA

Siciliano, SJ

Cascieri, MA

Carella, A

Carver, G

Holmes, K

Schleif, WA

Danzeisen, R

Hazuda, D

Kessler, J

Lineberger, J

Miller, M

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(02)00829-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as replacement of the benzylic methylene with sulfones, gem-difluoromethylenes and alcohols in an effort to balance the antiviral potency with reasonable pharmacokinetics. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：119 / 123

页数：5

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