Synthesis of novel derivatives of 4-methylbenzimidazole and evaluation of their biological activities

Eur J Med Chem. 2014 Sep 12:84:731-8. doi: 10.1016/j.ejmech.2014.07.078. Epub 2014 Jul 23.

Abstract

4-Methylbenzimidazole 1-28 novel derivatives were synthesized and evaluated for their antiglycation and antioxidant activities. Compounds 1-7 and 11 showed excellent activities ranged 140-280 μM, better than standard drug rutin (294.46 ± 1.50 μM). Compound 1-28 were also evaluated for DPPH activities. Compounds 1-8 showed excellent activities, ranging 12-29 μM, better than standard drug n-propylgallate (IC50 = 30.30 ± 0.40 μM). For superoxide anion scavenging activity, compounds 1-7 showed better activity than standard n-propylgallate (IC50 = 106.34 ± 1.6 μM), ranged 82-104 μM. These compounds were found to be nontoxic to THP-1 cells.

Keywords: Antiglycation; Antileishmanial; Antioxidant; Benzimidazole; Stereoisomers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antioxidants / chemical synthesis*
  • Antioxidants / chemistry
  • Antioxidants / pharmacology*
  • Antiprotozoal Agents / chemical synthesis*
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology*
  • Cell Line
  • Dose-Response Relationship, Drug
  • Glycosylation / drug effects
  • Humans
  • Leishmania / drug effects
  • Molecular Structure
  • Parasitic Sensitivity Tests

Substances

  • Antioxidants
  • Antiprotozoal Agents
  • Benzimidazoles