Study Of New Non-Thiazolidinediones PPAR-Agonist

The peroxisome proliferator-activated receptor (PPAR), a family member of the nuclear hormone receptor, plays a crucial role in regulating glycemia, insulin sensitivity and the storage and catabolism of dietary fats. Its subtype PPAR-γwas proved to be a key target for insulin sensitizers, such as thiazolidinedions (TZDs). Studies on novel selective PPAR-γagonist that retains efficacious insulin-sensitizing properties while minimizing potential adverse side effects have become a new direction to develop antidiabetes agents.Based on the SAR study of known TZDs, we designed three types of novel non-TZDs compounds with benzoxazole central structure which might have PPAR-γactivating potentials. We established several efficient synthetic methods and prepared eight new compounds. We have therefore validated a synthetic template for further research and development of antidiabetes drugs.