Abstract
The lipid-lowering activity of a series of novel N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives has been studied in Triton WR-1339-induced hyperlipidemia in rats. The test animals were divided into four groups: control, hyperlipidemic, compound + 4% DMSO [C1: N-(2-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (1), C2: N-(3-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (2), C3: N-(4-benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide (3)]-treated and bezafibrate (BF)-treated. At a dose of 15 mg/Kg body weight, compounds 2, 3 and BF significantly reduced elevated plasma triglycerodes levels after 12 h. Moreover, high density lipoprotein-cholesterol levels were significantly increased in all treated groups after 12 h compared to the hyperlipidemic control group, except for C1 which was inactive. In sum, it may be stated that the results of the present study demonstrated new properties of some N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives as potent lipid lowering agents and these beneficial activities may contribute to their cardioprotective and antiatherosclerotic role.
Highlights
Hyperlipidemia is defined as an elevation of lipids in plasma [1]
Several studies have showed that an intimate correlation exists between coronary heart diseases and hyperlipidemia [2,3], a rational approach to the treatment and prevention of coronary heart diseases could be by decreasing any elevated levels of lipids in plasma [4]
The major pharmacological mechanism of fibrates, including bezafibrate, is by the induction of lipoprotein lipase and reduction of apolipoprotein C-III synthesis leading to increased hydrolysis of triglycerides (TG) [9,10]
Summary
Several studies have showed that an intimate correlation exists between coronary heart diseases and hyperlipidemia [2,3], a rational approach to the treatment and prevention of coronary heart diseases could be by decreasing any elevated levels of lipids in plasma [4]. Triton WR-1339-induced hyperlipidemic rats are a globally accepted model used to evaluate potential hypolipidemic drugs [5]. A widely used class of lipid-modifying agents, results in a significant decrease in plasma triglycerides (79%) and is usually associated with a decrease in low density lipoprotein (LDL), cholesterol (11%), and an increase in high density lipoprotein (HDL)-cholesterol concentrations (27%) [8]. N-(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives have not been investigated as potential lipid-lowering agents. We aimed to synthesize a new series of ethyl-5fluoro-1H-indole-2-carboxamide derivatives and to investigate their hypolipidemic activity using.
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