Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists

被引：104

作者：

Zarrinmayeh, H ^{[1
]}

Zimmerman, DM ^{[1
]}

Cantrell, BE ^{[1
]}

Schober, DA ^{[1
]}

Bruns, RF ^{[1
]}

Gackenheimer, SL ^{[1
]}

Ornstein, PL ^{[1
]}

Hipskind, PA ^{[1
]}

Britton, TC ^{[1
]}

Gehlert, DR ^{[1
]}

机构：

[1] Eli Lilly & Co, Lilly Corp Ctr, Lilly Res Labs, Indianapolis, IN 46285 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(99)00082-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of benzimidazoles (4) was synthesized and evaluated in vitro as potent and selective NPY Y1 receptor antagonists. Substitution of the piperidine nitrogen of 4 with appropriate R groups resulted in compounds with more than 80-fold higher affinity at the Y1 receptor compared to the parent compound 5 (R = H). The most potent benzimidazole in this series was 21 (K-i = 0.052 nM). (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：647 / 652

页数：6

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