Synthesis and Antiinflammatory Activity of Some 3-(4,6-Disubstituted-2-thioxo--1,2,3,4-tetrahydropyrimidin-5-yl)propanoic Acid Derivatives. -Most of the synthesized novel propanoic acid derivatives (IV) show significant anti-inflammatory activity comparable to that of diclofenac. -(MOKALE*, S. N.; SHINDE, S. S.; ELGIRE, R. D.; SANGSHETTI, J. N.; SHINDE, D. B.; Bioorg. Med. Chem. Lett. 20 (2010) 15, 4424-4426,
A novel series of aminopyrimidines containing the phenoxy isobutyric acid group as a pharmacophore was synthesized using conventional and microwave assisted methods of synthesis. The compounds were synthesized in good yields (70-89%) by the microwave-assisted one-pot protocol in much shorter reaction times. The synthesized compounds were evaluated for their hypolipidemic and hypoglycemic activity by high-fat diet-induced hyperlipidemia and hyperglycemia in male Sprague-Dawley rats. The present investigation showed significant antihyperlipidemic and antihyperglycemic activity for all compounds of the series when compared with the standard drug. Structure-activity relationship (SAR) for the series were developed by comparing total lipid profile data of synthesized compounds with fenofibrate as standard drug.
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