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  • Title: Synthesis and biological activity of novel pyrimidinone containing thiazolidinedione derivatives.
    Author: Madhavan GR, Chakrabarti R, Vikramadithyan RK, Mamidi RN, Balraju V, Rajesh BM, Misra P, Kumar SK, Lohray BB, Lohray VB, Rajagopalan R.
    Journal: Bioorg Med Chem; 2002 Aug; 10(8):2671-80. PubMed ID: 12057656.
    Abstract:
    A series of pyrimidinone derivatives of thiazolidinediones were synthesized. Their biological activity were evaluated in insulin resistant, hyperglycemic and obese db/db mice. In vitro PPARgamma transactivation assay was performed in HEK 293T cells. PMT13 showed the best biological activity in this series. PMT13 (5-[4-[2-[2-ethyl-4-methyl-6-oxo-1,6-dihydro-1-pyrimidinyl]ethoxy]phenylmethyl]thiazolidine-2,4-dione) showed better plasma glucose, triglyceride and insulin-lowering activity in db/db mice than rosiglitazone and pioglitazone. PMT13 showed better PPARgamma transactivation than the standard compounds. Pharmacokinetic study in Wistar rats showed good systemic exposure of PMT13. Twenty-eight day oral toxicity study in Wistar rats did not show any treatment-related adverse effects.
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