- Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists
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A series of substituted chromones were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor 1. Compounds with subnanomolar binding affinity and 66% oral bioavailability in rats were discovered.
- Dyck, Brian,Zhao, Liren,Tamiya, Junko,Pontillo, Joseph,Hudson, Sarah,Ching, Brett,Heise, Christopher E.,Wen, Jenny,Norton, Christi,Madan, Ajay,Schwarz, David,Wade, Warren,Goodfellow, Val S.
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p. 4237 - 4242
(2007/10/03)
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- 2- (3-AMINOPYRROLIDIN-1-YL) PYRIDINES AS MELANIN-CONCENTRATING HORMONE RECEPTOR AN TAGONISTS
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Melanin-concentrating hormone (MCH) receptor antagonists are disclosed having utility for the treatment of MCH receptor-based disorders such as obesity. The compounds of this invention have the following structure: including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein R1, R2, R5, Het, X and Cyc are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.
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Page/Page column 28
(2010/02/14)
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