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
收藏
页码：1795 / 1798
页数：4
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