Benzotriazole: An overview on its versatile biological behavior

Eur J Med Chem. 2015 Jun 5;97:612-48. doi: 10.1016/j.ejmech.2014.09.089. Epub 2014 Sep 30.


Discovered in late 1960, azoles are heterocyclic compounds class which constitute the largest group of available antifungal drugs. Particularly, the imidazole ring is the chemical component that confers activity to azoles. Triazoles are obtained by a slight modification of this ring and similar or improved activities as well as less adverse effects are reported for triazole derivatives. Consequently, it is not surprising that benzimidazole/benzotriazole derivatives have been found to be biologically active. Since benzimidazole has been widely investigated, this review is focused on defining the place of benzotriazole derivatives in biomedical research, highlighting their versatile biological properties, the mode of action and Structure Activity Relationship (SAR) studies for a variety of antimicrobial, antiparasitic, and even antitumor, choleretic, cholesterol-lowering agents.

Keywords: 1H-benzo[d][1,2,3]triazole; Anti-tubulin; Antimicrobial; Antimycobacterial; Antiprotozoal; Antiviral.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Discovery / methods*
  • Humans
  • Triazoles / pharmacology*


  • Triazoles
  • benzotriazole