Synthesis, Antibacterial, and Anti HepG2 Cell Line Human Hepatocyte Carcinoma Activity of Some New Potentially Benzimidazole-5-(Aryldiazenyl)Thiazole Derivatives

Molecules. 2018 Dec 11;23(12):3285. doi: 10.3390/molecules23123285.

Abstract

The paper describes the synthesis and biological evaluation of some new benzimidazole derivatives as potent clinical drugs that are useful in the treatment of some microbial infections and tumor inhibition. The starting compound 2-(bromomethyl)-1H-benzimidazole (1) was prepared, and hence underwent interesting functionalization reactions to afford several series of benzimidazole-5-(aryldiazenyl)thiazole derivatives: 3ac, 7ac, and 8ac. The antibacterial activities of the synthesized compounds were evaluated by calculation of the inhibition zone diameter (mm) and the determination of minimum inhibitory concentration (µg/mL) against selected pathogenic bacteria Staphylococcus aureus (Gram-positive bacteria) and Escherichia coli (Gram-negative bacteria).Noticeable efficiency was found based on in vitro screening for their antioxidant activity and cytotoxicity effect against the human liver cancer cell line (HepG2) and human hepatocyte carcinoma cells at relatively high concentrations.

Keywords: HepG2 cell line; antimicrobial activity; antitumor; benzimidazoles; pathogenic bacteria.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Benzimidazoles / chemistry
  • Drug Evaluation, Preclinical / methods
  • Escherichia coli / drug effects
  • Hep G2 Cells
  • Humans
  • Microbial Sensitivity Tests
  • Staphylococcus aureus / drug effects
  • Thiazoles / chemistry

Substances

  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Antioxidants
  • Benzimidazoles
  • Thiazoles