Co-crystal structure guided array synthesis of PPARγ inverse agonists

PPARγ-activating thiazolidinediones and carboxylic acids such as farglitazar exert their anti-diabetic effects in part in PPARγ rich adipose. Both pro- and anti-adipogenic PPARγ ligands promote glucose and lipid lowering in animal models of diabetes. Herein, we disclose representatives of an array of 160 farglitazar analogues with atypical inverse agonism of PPARγ in mature adipocytes.

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