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

…, BM Rajesh, V Balraju, PB Rao, R Rajagopalan…

文献索引：Madhavan, Gurram R.; Chakrabarti, Ranjan; Anantha Reddy; Rajesh; Balraju; Bheema Rao; Rajagopalan; Iqbal, Javed Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 2 p. 584 - 591

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被引用次数: 47

摘要

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.