Bioorganic & Medicinal Chemistry Letters 2006-09-15

The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.

Donald L Hertzog, Kamal A Al-Barazanji, Eric C Bigham, 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, Huiqiang Zhou

Index: Bioorg. Med. Chem. Lett. 16(18) , 4723-27, (2006)

Full Text: HTML

Abstract

Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) 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.