Dual PPAR-α and -γ activators derived from novel benzoxazinone containing thiazolidinediones having antidiabetic and hypolipidemic potential

2,4-Thiazolidinedione derivatives of 1,3-benzoxazinone were synthesized and evaluated for their PPAR-α and -γ dual activation. DRF-2519, a compound obtained through SAR of TZD derivatives of benzoxazinone, has shown potent dual PPAR activation. In ob/ob mice, it showed better efficacy than the comparator molecules. In fat fed rat model, it showed significant improvement in lipid parameters, which was better than fibrates.

Synthesis, SAR study, and biological evaluation of a new series of 1,3-4(3H)benzoxazinone derivatives of thiazolidinedione are reported.Figure optionsDownload as PowerPoint slide