Abstract: In the search for new potential antihyperlipidemic agents, the present study focuses on the synthesis of novel N-(benzoylphenyl)-5-substituted-1H-indole-2-carboxamides (compounds 8-12, 15, 16, 18) and investigating their antihyperlipidemic activity using Triton WR-1339-induced hyperlipidemic rats as an experimental model. Hyperlipidemia was developed by intraperitoneal injection of Triton WR-1339 (250 mg/kg body weight). The tested animals were divided into normal control (NCG), hyperlipidemic (HG), compound 8, 9, 15, 16, 18- and bezafibrate treated groups. At a dose of 15 mg/kg body weight, compounds 9, 16, 18 and bezafibrate (100 mg/kg) significantly (p < 0.0001) reduced elevated plasma triglycerides levels after 12 h compared to the hyperlipidemic control group. However, only the group treated with compounds 9, 16 and 18 showed an obviously significant (p < 0.001) reduction in plasma total cholesterol levels after 12 h compared to the hyperlipidemic control group. Moreover, high density lipoprotein-cholesterol levels were significantly (p < 0.0001) increased in all treated groups after 12 h compared to the hyperlipidemic control group, except for compounds 8 and 15 which revealed inactive. It is therefore reasonable to assume that compounds 9, 16 and 18 may have potential in the treatment of hyperlipidemia.
Keywords: Triton WR-1339-induced hyperlipidemic rats; N-(benzoylphenyl)-5-methoxy-1H-indole-2-carboxamide; N-(Benzoylphenyl)-5-chloro-1H-indole-2-carboxamide; hypo-lipidemic activity
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Al-Hiari, Y.; Shattat, G.; Al-Qirim, T.; El-Huneidi, W.; Sheikha, G.A.; Hikmat, S. Antihyperlipidemic Properties of Novel N-(Benzoylphenyl)-5-substituted-1H-indole-2-carboxamides in Triton WR-1339-Induced Hyperlipidemic Rats. Molecules 2011, 16, 8292-8304.
Al-Hiari Y, Shattat G, Al-Qirim T, El-Huneidi W, Sheikha GA, Hikmat S. Antihyperlipidemic Properties of Novel N-(Benzoylphenyl)-5-substituted-1H-indole-2-carboxamides in Triton WR-1339-Induced Hyperlipidemic Rats. Molecules. 2011; 16(10):8292-8304.
Al-Hiari, Yusuf; Shattat, Ghassan; Al-Qirim, Tariq; El-Huneidi, Waseem; Sheikha, Ghassan Abu; Hikmat, Suhair. 2011. "Antihyperlipidemic Properties of Novel N-(Benzoylphenyl)-5-substituted-1H-indole-2-carboxamides in Triton WR-1339-Induced Hyperlipidemic Rats." Molecules 16, no. 10: 8292-8304.