3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.
作者： Gino Salituro , Andrew D. Howard , Sander G. Mills , Lihu Yang , Shawn P. Walsh
DOI: 10.1016/J.BMCL.2011.03.114
关键词:
摘要: 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 the pendant aryloxy group led to identification potent agonists. In order identify candidates suitable in vivo validation target, serum shifted potency pharmacokinetic properties were determined several compounds. Finally, further profiling compound 7 presented, including demonstration enhanced glucose tolerance an mouse model.
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