Synthesis of benzothiophene carboxamide derivatives and their pharmacological evaluation as potent antihypertriglyceridemic agents in rats

摘要

Benzothiophene carboxamide derivatives of aminobenzophenone, aminopyridine, aminobenzimidazole, and aniline derivatives (compounds 1 - 9) were synthesized and compounds 3, 6, 7, 8, and 9 tested in vivo for their hypolipidemic activity. Compounds 1 - 8 were prepared adopting the fusion process at 130 - 150 °C between benzothiophene-2-carbonyl chloride and aminobenzophenones, aminopyridine, and anilines, respectively, and were obtained in high yield, while compound 9 was obtained from the reaction of benzothiophene acyl chloride with aminobenzimidazole in DMF at 160 °C. At a dose of 15 mg/kg body weight compounds 6, 7, and 9 significantly reduced plasma triglyceride levels in Triton WR-1339-induced hyperlipidemic rats in comparison to control rats. Furthermore, they significantly increased high-density lipoprotein levels. It is therefore reasonable to assume that compounds 6, 7, and 9 may have a promising potential in the treatment of hyperlipidemia and atherosclerosis.