Antihyperlipidemic properties of novel N-(benzoylphenyl)-5-substituted-1H-indole-2-carboxamides in Triton WR-1339-induced hyperlipidemic rats

Molecules. 2011 Sep 29;16(10):8292-304. doi: 10.3390/molecules16108292.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bezafibrate / pharmacology
  • Cholesterol, HDL / blood
  • Hyperlipidemias / blood
  • Hyperlipidemias / chemically induced
  • Hyperlipidemias / drug therapy*
  • Hypolipidemic Agents / chemical synthesis
  • Hypolipidemic Agents / chemistry*
  • Hypolipidemic Agents / pharmacology*
  • Indoles / chemical synthesis
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Male
  • Polyethylene Glycols
  • Rats
  • Rats, Wistar
  • Triglycerides / blood

Substances

  • Cholesterol, HDL
  • Hypolipidemic Agents
  • Indoles
  • N-(benzoylphenyl)-5-chloro-1H-indole-2-carboxamide
  • N-(benzoylphenyl)-5-methoxy-1H-indole-2-carboxamide
  • Triglycerides
  • Polyethylene Glycols
  • tyloxapol
  • Bezafibrate