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.
Highlights
Cardiovascular diseases are the most common cause of death in developed countries [1].Hyperlipidemia is defined as elevation of one or more of the plasma lipids, including triglycerides, cholesterol, cholesterol esters and phospholipids [2]
Triton WR-1339-induced hyperlipidemic rats are widely used as a model to screen for or to differentiate the mechanism of action of potential hypolipidemic agents [9,10,11]
Given the importance in fighting hyperlipidemia, which is the prevalent risk of cardiovascular diseases, the present study focuses on the synthesis (Schemes 1 and 2) and pharmacological evaluation of novel N-(benzoylphenyl)-5-substituted-1H-indole-2-carboxamide derivatives from 5-methoxy- and
Summary
Cardiovascular diseases are the most common cause of death in developed countries [1]. Hyperlipidemia is defined as elevation of one or more of the plasma lipids, including triglycerides, cholesterol, cholesterol esters and phospholipids [2] This pathological condition has been ranked as one of the most important risk factors contributing to the occurrence and severity of cardiovascular diseases [3,4]. Triton WR-1339-induced hyperlipidemic rats are widely used as a model to screen for or to differentiate the mechanism of action of potential hypolipidemic agents [9,10,11] Fibrates and their derivatives are group of drugs, which have been widely used to treat hyperlipoproteinemia, in particular cases with elevated TG. Given the importance in fighting hyperlipidemia, which is the prevalent risk of cardiovascular diseases, the present study focuses on the synthesis (Schemes 1 and 2) and pharmacological evaluation of novel N-(benzoylphenyl)-5-substituted-1H-indole-2-carboxamide derivatives from 5-methoxy- and. Cl i: SOCl2, DCM, 70–80 °C, 20hr, ii: acetonitrile, toluene, 110–120 °C, 20–24 hrs
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