Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.

Vincent Mascitti,Benjamin D Stevens,Chulho Choi,Kim F McClure,Cristiano R W Guimarães,Kathleen A Farley,Michael J Munchhof,Ralph P Robinson,Kentaro Futatsugi,Sophie Y Lavergne,Bruce A Lefker,Peter Cornelius,Paul D Bonin,Amit S Kalgutkar,Raman Sharma,Yue Chen

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

The design and synthesis of a GPR119 agonist bearing a 2-(2,3,6-trifluorophenyl)acetamide group is described. The design capitalized on the conformational restriction found in N-β-fluoroethylamide derivatives to help maintain good levels of potency while driving down both lipophilicity and oxidative metabolism in human liver microsomes. The chemical stability and bioactivation potential are discussed.

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关键词

GPR119,Diabetes,Gauche effect,Configurational entropy,Metabolism

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