Synthesis of Novel Benzimidazole-2-carboxamide Derivatives and in Vivo Antihyperlipidemic Activity Evaluation

Chem Pharm Bull (Tokyo). 2018;66(4):423-426. doi: 10.1248/cpb.c17-00908.

Abstract

Hyperlipidemia is known as an elevation of plasma lipid components. It contributes significantly to atherosclerosis which is one of the most important causative factors in cardiovascular diseases. Agents that cause a dramatic decrease in serum lipid levels are of great value in the treatment of cardiovascular diseases. For this purpose, a new series of benzimidazole propyl carboxamide benzophenone derivatives have been synthesized (7, 8, and 9). These compounds were tested in vivo to evaluate their potential hypolipidemic activity using Triton WR-1339 induced hyperlipidemic rats. All the synthesized compounds have proved to be highly biologically active, with compound 9 being the most active derivative.

Keywords: Triton WR-1339; benzimidazole; cardiovascular disease; hyperlipidemia; low-density lipoprotein (LDL).

MeSH terms

  • Animals
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Hyperlipidemias / chemically induced
  • Hyperlipidemias / drug therapy*
  • Hypolipidemic Agents / chemical synthesis
  • Hypolipidemic Agents / chemistry
  • Hypolipidemic Agents / pharmacology*
  • Injections, Intraperitoneal
  • Male
  • Molecular Structure
  • Polyethylene Glycols / administration & dosage
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship

Substances

  • Benzimidazoles
  • Hypolipidemic Agents
  • Polyethylene Glycols
  • tyloxapol