Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists

被引:43
作者
Arienzo, R [1 ]
Clark, DE [1 ]
Cramp, S [1 ]
Daly, S [1 ]
Dyke, HJ [1 ]
Lockey, P [1 ]
Norman, D [1 ]
Roach, AG [1 ]
Stuttle, K [1 ]
Tomlinson, M [1 ]
Wong, M [1 ]
Wren, SP [1 ]
机构
[1] Argenta Discovery Ltd, Harlow CM19 5TR, Essex, England
关键词
D O I
10.1016/j.bmcl.2004.05.051
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new series of 2-aminoquinolines has been identified as antagonists of the melanin concentrating hormone receptor (MCH-1R). Syntheses and structure-activity relationships are described leading to a compound having low nanomolar activity against the receptor and demonstrating functional antagonism. Studies also showed that some of the compounds were selective against a range of other G protein-coupled receptors. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4099 / 4102
页数:4
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