In vivo antihyperlipidemic activity of a new series of N-(benzoylphenyl) and N-(acetylphenyl)-1-benzofuran-2-carboxamides in rats

Arch Pharm (Weinheim). 2012 May;345(5):401-6. doi: 10.1002/ardp.201100225. Epub 2012 Jan 20.

Abstract

A new series of N-(benzoylphenyl) and N-(acetylphenyl)-1-benzofuran-2-carboxamides (3a-3d and 4a'-4c') were synthesized. Compounds (3a, 3b, and 4a'-4c') were tested in vivo using Triton-WR-1339-induced hyperlipidemic rats as an experimental model for their hypolipidemic activity. The tested animals were divided into eight groups: control, hyperlipidemic, 3a, 3b, 4a', 4b', 4c', and bezafibrate. At a dose of 15 mg/kg, the elevated plasma triglyceride (TG) levels were significantly reduced in compounds 3b (p <0.0001) and 4c' (p <0.05) after 12 and 24 h compared to the normal control group. Furthermore, high-density lipoprotein-cholesterol levels were remarkably increased in compounds 3b (p <0.001) and 4c' (p <0.05). Meanwhile, compound 4b' slightly reduced the TG levels after 12 and 24 h. The present study demonstrated new properties of the novel series of benzofuran-2-carboxamides 3b and 4c' as potent lipid-lowering agents. It is, therefore, reasonable to assume that compounds 3b and 4c' may have a promising potential in the treatment of hyperlipidemia and coronary heart diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzofurans / chemical synthesis*
  • Benzofurans / pharmacology
  • Bezafibrate / pharmacology
  • Cholesterol, HDL / blood
  • Cholesterol, LDL / blood
  • Hypolipidemic Agents / chemical synthesis*
  • Hypolipidemic Agents / pharmacology
  • Male
  • Polyethylene Glycols
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship
  • Triglycerides / blood

Substances

  • Benzofurans
  • Cholesterol, HDL
  • Cholesterol, LDL
  • Hypolipidemic Agents
  • Triglycerides
  • Polyethylene Glycols
  • tyloxapol
  • Bezafibrate