We have discovered that (-)-Cercosporamide, known as an antifungal agent and phytotoxin, showed a glucose lowering effect in hyperglycemic mice. In synthesizing the derivatives and investigating the mechanisms of action, we have noticed that some of the derivatives resulted in a PPAR? partial agonistic effect. We would like to display a detailed SAR study on the PPAR? modulators and in vivo efficacies of the most promising compound, decreasing the plasma glucose level with attenuated PPAR? related adverse effects.

Discovery of novel (−)-Cercosporamide derivatives as selective PPARγ modulators

243rd National Meeting (2012)

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