Synthesis and anti-hyperlipidemic evaluation of N‑(benzoylphenyl)-5-fluoro-1H-indole-2-carboxamide derivatives in Triton WR-1339-induced hyperlipidemic rats

Molecules. 2010 Aug 26;15(9):5840-9. doi: 10.3390/molecules15095840.

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.

MeSH terms

  • Animals
  • Bezafibrate / pharmacology
  • Bezafibrate / therapeutic use
  • Cholesterol, HDL / blood
  • Hyperlipidemias / chemically induced
  • Hyperlipidemias / drug therapy*
  • Hypolipidemic Agents / chemical synthesis*
  • Hypolipidemic Agents / pharmacology*
  • Hypolipidemic Agents / therapeutic use
  • Indoles / chemical synthesis*
  • Indoles / pharmacology*
  • Indoles / therapeutic use
  • Male
  • Polyethylene Glycols / metabolism
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship

Substances

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