The Discovery And Optimization Of Pyrimidinone-Containing Mch R1 Antagonists

Donald L. Hertzog,Kamal-A. Al-Barazanji, Eric C. Bigharn,Michael J. Bishop,Christy S. Britt,David L. Carlton,Joel P. Cooper, Alex J. Daniels,Dulce M. Garrido,Aaron S. Goetz,Mary K. Grizzle,Yu C. Guo,Anthony L. Handlon,Diane M. Ignar,Ronda O. Morgan,Andrew J. Peat,Francis X. Tavares,Huqiang Zhou

Bioorganic & medicinal chemistry letters（2006）

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摘要

Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH RI) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided and the use of one of the compounds in an animal model of diet-induced obesity is presented. (c) 2006 Elsevier Ltd. All rights reserved.

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melanin-concentrating hormone,MCH,MCH R1,MCH antagonist,MCH R1 antagonist

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