INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH AND BIO-SCIENCE

In this letter, the series of isoxazole triple bond propanoic acid compounds design, synthesis, structure-activity relationship (SAR) and the ability to modulate the activity of GPR40 are described. The Systematic replacement of substituted aryl groups, various substitutions on isoxazole and optimization of chain length led to identification of potent GPR40 agonists. In order to identify candidate suitable for in vivo validation of the target, pharmacokinetic properties were determined and further profiling of the compound is presented. The compound 1 may prove useful for the treatment of Type 2 diabetes.