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  • Title: Dual PPAR-alpha and -gamma activators derived from novel benzoxazinone containing thiazolidinediones having antidiabetic and hypolipidemic potential.
    Author: Madhavan GR, Chakrabarti R, Reddy KA, Rajesh BM, Balraju V, Rao PB, Rajagopalan R, Iqbal J.
    Journal: Bioorg Med Chem; 2006 Jan 15; 14(2):584-91. PubMed ID: 16198573.
    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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