1-(4-amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists

被引：33

作者：

Huang, CQ

Baker, T

Schwarz, D

Fan, J

Heise, CE

Zhang, MZ

Goodfellow, VS

Markison, S

Gogas, KR

Chen, TK

Wang, XC

Zhu, YF

机构：

[1] Neurocrine Biosci Inc, Dept Med Chem, San Diego, CA 92130 USA

[2] Neurocrine Biosci Inc, Dept Biol Mol, San Diego, CA 92130 USA

[3] Neurocrine Biosci Inc, Dept Pharmacol, San Diego, CA 92130 USA

[4] Neurocrine Biosci Inc, Dept Neurosci, San Diego, CA 92130 USA

[5] Neurocrine Biosci Inc, Dept Preclin Dev, San Diego, CA 92130 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 16期

关键词：

D O I：

10.1016/j.bmcl.2005.05.130

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Derivatives of 1-(4-amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine were identified as potent and functionally active MCH-R1 antagonists. One compound with K-i = 2.3 nM demonstrated good oral bioavailability (32%) and in vivo efficacy in rats. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：3701 / 3706

页数：6

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