CCR5 antagonists:: Bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines

被引：36

作者：

Lynch, CL

Gentry, AL

Hale, JJ

Mills, SG

MacCoss, M

Malkowitz, L

Springer, MS

Gould, SL

DeMartino, JA

Siciliano, SJ

Cascieri, MA

Doss, G

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 Drug Metab, NMR Spect, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Antiviral Res, W Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(01)00835-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of CCR5 antagonists containing bicyclic isoxazolidines was generated through a nitrone mediated cycloaddition with olefins bearing the preferred pharmacophores previously described. Potent antagonists (3 and 16) were generated with enhanced affinity for the CCR5 receptor while maintaining antiviral activity against HIV. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：677 / 679

页数：3

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