3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists

SP Walsh, A Severino, C Zhou, J He, GB Liang…

文献索引：Walsh, Shawn P.; Severino, Alexandra; Zhou, Changyou; He, Jiafang; Liang, Gui-Bai; Tan, Carina P.; Cao, Jin; Eiermann, George J.; Xu, Ling; Salituro, Gino; Howard, Andrew D.; Mills, Sander G.; Yang, Lihu Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3390 - 3394

全文：HTML全文

被引用次数: 19

摘要

Abstract The design, synthesis, and structure–activity relationship (SAR) for a series of β- substituted 3-(4-aryloxyaryl) propanoic acid GPR40 agonists is described. Systematic replacement of the pendant aryloxy group led to identification of potent GPR40 agonists. In order to identify candidates suitable for in vivo validation of the target, serum shifted potency and pharmacokinetic properties were determined for several compounds. Finally, further ...