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BY-NC-ND 3.0 license Open Access Published by De Gruyter June 2, 2014

Synthesis of Benzothiophene Carboxamide Derivatives and their Pharmacological Evaluation as Potent Antihypertriglyceridemic Agents in Rats

  • Ghassan Abu Sheikha , Buthina Hussin , Yusuf Al-Hiari , Tariq Al-Qirim EMAIL logo and Ghassan Shattat

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

Received: 2010-7-1
Revised: 2010-11-8
Published Online: 2014-6-2
Published in Print: 2011-4-1

© 1946 – 2014: Verlag der Zeitschrift für Naturforschung

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