- Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1)
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A novel series of bis-aminopyrrolidine ureas containing either a 4-biphenylcarboxmide or 5-phenyl-2-thiophenecarboxamide group have been identified as potent and functional antagonists of the melanin-concentrating hormone receptor-1. Syntheses and SAR are
- Rowbottom, Martin W.,Vickers, Troy D.,Dyck, Brian,Tamiya, Junko,Zhang, Mingzhu,Zhao, Liren,Grey, Jonathan,Provencal, David,Schwarz, David,Heise, Christopher E.,Mistry, Monica,Fisher, Andrew,Dong, Teresa,Hu, Tao,Saunders, John,Goodfellow, Val S.
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p. 3439 - 3445
(2007/10/03)
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- Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists
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Ureas derived from two substituted 3-aminopyrrolidine subunits were prepared as constrained analogs of a linear lead compound and tested as antagonists of the MCH1 receptor. The series was optimized for substitution and stereochemistry to generate a functional antagonist with a Ki of 3.3 nM and IC50 of 12 nM (GTPγS).
- Grey, Jonathan,Dyck, Brian,Rowbottom, Martin W.,Tamiya, Junko,Vickers, Troy D.,Zhang, Mingzhu,Zhao, Liren,Heise, Christopher E.,Schwarz, David,Saunders, John,Goodfellow, Val S.
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p. 999 - 1004
(2007/10/03)
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- MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISTS AND COMPOSITIONS AND METHODS RELATED THERETO
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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 m, n, X, R1, R2, R3, R4, and R5 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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