Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists

被引:9
作者
Balavoine, Fabrice
Malabre, Patrice
Alleaume, Thierry
Rey, Astrid
Cherfils, Valerie
Jeanneton, Olivier
Seigneurin-Venin, Sophie
Revah, Frederic
机构
[1] CEREP, F-91951 Villebrumier, France
[2] Cerep, F-86600 Celle Levescault, France
关键词
hydantoin; melanin-concentrating hormone; MCHR-1; antagonists; obesity; feeding; depression;
D O I
10.1016/j.bmcl.2007.04.012
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor I (MCHR-1). Synthesis and structure-activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity has been demonstrated in animal models of food intake and depression. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3754 / 3759
页数:6
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