Synthesis and pharmacological study of antihyperlipaemic activity of 2-substituted thieno(2,3-d)pyrimidin-4(3H)-ones.

Abstract

A series of 2-substituted thieno(2,3-d)pyrimidin-4-(3H) ones (1-15) was prepared by the reaction of thiophene ortho-aminoester (IV) with a variety of nitriles (V) under acidic conditions, and screened for antihyperlipaemic activity in various animal models. While most of these compounds were found active, 2-chloromethyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d) pyrimidin-4(3H)-one (5) was found to be the most active of all. The serum triglyceride lowering activity exhibited by 5 was found comparable to that of clofibrate and riboflavin tetrabutyrate. Compound 5 was also found to be safe as indicated by acute and chronic toxicity studies in mice and rats.

Cite this paper

@article{Shishoo1990SynthesisAP, title={Synthesis and pharmacological study of antihyperlipaemic activity of 2-substituted thieno(2,3-d)pyrimidin-4(3H)-ones.}, author={Chamanlal J Shishoo and Muljibhai B. Devani and Vishweshwar S Bhadti and Kishor S. Jain and Ishwarsinh S Rathod and Ramesh Kishorilal Goyal and Tripti Gandhi and Rameshkumar B Patel and Suresh Ramnath Naik}, journal={Arzneimittel-Forschung}, year={1990}, volume={40 5}, pages={567-72} }