The biology and chemistry of antifungal agents: a review

Bioorg Med Chem. 2012 Oct 1;20(19):5678-98. doi: 10.1016/j.bmc.2012.04.045. Epub 2012 May 9.


In recent years their has been an increased use of antifungal agents and has resulted in the development of resistance to drugs. Currently, use of standard antifungal therapies can be limited because of toxicity, low efficacy rates. Different types of mechanisms contribute to the development of resistance to antifungals. This has given raise to search for a new heterocycle with distinct action or multitargeted combination therapy. This review addresses the areas such as the underlying mechanisms, eight different targets such as ergosterol synthesis, chitin synthesis, ergosterol disruptors, glucan synthesis, squalene epoxidase, nucleic acid synthesis, protein synthesis, microtubules synthesis. The clinically employed drugs along with the current research work going on worldwide on different heterocycles are discussed. In recent advances various heterocycles including imidazole, benzimidazole etc., twenty three scaffolds and their lead identification are discussed.

Publication types

  • Review

MeSH terms

  • Animals
  • Antifungal Agents / chemistry*
  • Antifungal Agents / pharmacology*
  • Antifungal Agents / therapeutic use
  • Azoles / chemistry
  • Azoles / pharmacology
  • Azoles / therapeutic use
  • Fungi / drug effects*
  • Fungi / metabolism
  • Humans
  • Imidazoles / chemistry
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use
  • Mycoses / drug therapy*


  • Antifungal Agents
  • Azoles
  • Imidazoles