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

Synthesis and Pharmacological Evaluation of Novel Substituted and Unsubstituted N-(Benzoylphenyl)-1H-indole-2-carboxamides as Potent Antihypertriglyceridemic Agents

  • Moyad Shahwan , Ghassan Shattat , Tariq Al-Qirim EMAIL logo , Ghassan Abu Sheikha , Yusuf Al-Hiari , Waseem El-Huneidi , Anan Jarab and Manal Al-Najdawi

The N-(benzoylphenyl)-1H-indole-2-carboxamide derivatives 1 - 6 were synthesized, and the lipid-lowering effects of two of these novel compounds were studied using hyperlipidemic rats as an experimental model. Treatment of ethyl-1H-indole-2-carboxylate with aminobenzophenones in the presence of sodium ethoxide and DMF, followed by purifi cation using column chromatography, gave the target compounds in good yields. The tested animals were divided into control, hyperlipidemic, compounds 2-, 3- and bezafibrate-treated groups. At a dose of 15 mg/kg body weight, compounds 2, 3 and bezafibrate significantly reduced the elevated plasma triglyceride levels after 7 and 24 h. Furthermore, the high-density lipoprotein- cholesterol levels were remarkably increased in all treated groups after 7 and 24 h compared to the hyperlipidemic control group. However, only compounds 2- and 3-treated groups obviously showed a significant reduction in plasma total cholesterol levels after 24 h. It is therefore reasonable to assume that 2 and 3 may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.

Received: 2009-11-15
Revised: 2010-1-14
Published Online: 2014-6-2
Published in Print: 2010-6-1

© 1946 – 2014: Verlag der Zeitschrift für Naturforschung

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