Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists

被引：21

作者：

Jiang, JL

DeVita, RJ

Goulet, MT

Wyvratt, WJ

Lo, JL

Ren, N

Yudkovitz, JB

Cui, JS

Yang, YT

Cheng, K

Rohrer, SP

机构：

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

[2] Merck Res Labs, Dept Atherosclerosis & Endocrinol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 07期

关键词：

D O I：

10.1016/j.bmcl.2003.12.101

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Syntheses and structure-activity relationships of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists are described. Some of substituents on the piperidine ring that were investigated included a fused phenyl group, a (6R)-trifluoromethyl group, (6S) and (6R)-methyl group. This study showed that GnRH binding potency was tolerated by a small group at the 6-position of the piperidine, and blocking the 6-position by a trifluoromethyl group reduced clearance rate and increased oral bioavailability. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：1795 / 1798

页数：4

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