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. 2006 Jan 15;14(2):584-91.
doi: 10.1016/j.bmc.2005.08.043. Epub 2005 Sep 28.

Dual PPAR-alpha and -gamma activators derived from novel benzoxazinone containing thiazolidinediones having antidiabetic and hypolipidemic potential

Gurram R Madhavan  1 , Ranjan Chakrabarti, K Anantha Reddy, B M Rajesh, V Balraju, P Bheema Rao, R Rajagopalan, Javed Iqbal
Affiliations

Dual PPAR-alpha and -gamma activators derived from novel benzoxazinone containing thiazolidinediones having antidiabetic and hypolipidemic potential

Gurram R Madhavan et al. Bioorg Med Chem. .

Abstract

2,4-Thiazolidinedione derivatives of 1,3-benzoxazinone were synthesized and evaluated for their PPAR-alpha and -gamma 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.

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