Abstract
AbstractThe G‐protein‐coupled receptor 40 (GPR40) plays an important role in glucose‐stimulated insulin secretion and therefore may be a promising anti‐diabetic target. In this study, we have replaced the phenylpropionic acid of GPR40 agonist GW9508 with phenylacetic acid to avoid β‐oxidation. The molecular modeling study based on phenylacetic acid scaffold suggested that the present series fitted very well with the binding pocket of GPR40. Further structure‐activity relationship study provided the optimal compound 6, which revealed better in vivo hypoglycemic effect than GW9508 both in normal and type 2 diabetic mice. These findings suggested that compound 6 was meaningful for further investigation and highlighted its potential as a lead compound.
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