| Literature DB >> 12057656 |
Gurram R Madhavan1, Ranjan Chakrabarti, Reeba K Vikramadithyan, Rao N V S Mamidi, V Balraju, B M Rajesh, Parimal Misra, Sunil K B Kumar, Braj B Lohray, Vidya B Lohray, Ramanujam Rajagopalan.
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.Entities:
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Year: 2002 PMID： 12057656 DOI： 10.1016/s0968-0896(02)00107-4
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641