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Antifungal Agents

  1. William J. Watkins,
  2. Thomas E. Renau

Published Online: 15 JAN 2003

DOI: 10.1002/0471266949.bmc090

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Watkins, W. J. and Renau, T. E. 2003. Antifungal Agents. Burger's Medicinal Chemistry and Drug Discovery. 881–918.

Author Information

  1. Essential Therapeutics, Mountain View, California, USA

Publication History

  1. Published Online: 15 JAN 2003


The chapter addresses current chemotherapeutic options and trends in the treatment of fungal diseases in humans. The nature of such diseases is discussed, with attendant issues such as relative severity, diagnosis, microbiological methods, and trends in incidence. Emphasis is placed on systemic infections, in which morbidity and mortality are much higher than that in cutaneous diseases. The various drugs with proven clinical utility are then surveyed by chemical class, with a discussion of mode of action, spectrum and emergence of resistance, pharmacokinetic properties, and side effects for each; for the most prominent class of antifungal agents (the azoles), the history of their medicinal evolution is described. Where appropriate, comment is made about new developments in the field with a brief summary of newer agents in clinical development. Also included is a section reviewing chemical series with interesting (and selective) modes of action that have not yet been tested clinically. Finally, the anticipated impact of new technologies on antifungal drug discovery is briefly discussed.


  • antifungal;
  • Candida spp;
  • Aspergillus spp;
  • candidiasis;
  • aspergillosis;
  • ergosterol biosynthesis;
  • fungal cell wall;
  • polyenes;
  • azoles;
  • allylamines;
  • candins;
  • thiocarbamates;
  • morpholines;
  • flucytosine;
  • griseofulvin;
  • nikkomycin;
  • aureobasidin;
  • sordarins;
  • pradimicins;
  • benanamycins;
  • N-myristoyl transferase inhibitors;
  • fungal efflux pump inhibitors