Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones

J Med Chem. 1984 Jul;27(7):894-900. doi: 10.1021/jm00373a015.

Abstract

A series of novel triazol-3-ones have been synthesized, and their in vitro and in vivo antifungal properties are reported. Compound 68 (itraconazole), which displays a pronounced oral activity against vaginal candidosis in rats and against microsporosis in guinea pigs, has been selected for clinical evaluation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antifungal Agents / chemical synthesis*
  • Aspergillus fumigatus / drug effects
  • Candida / drug effects
  • Candidiasis, Vulvovaginal / drug therapy
  • Cryptococcus neoformans / drug effects
  • Dermatomycoses / drug therapy
  • Female
  • Guinea Pigs
  • Itraconazole
  • Ketoconazole / analogs & derivatives*
  • Ketoconazole / chemical synthesis
  • Ketoconazole / therapeutic use
  • Microsporum / drug effects
  • Phialophora / drug effects
  • Rats
  • Rats, Inbred Strains
  • Sporothrix / drug effects
  • Triazoles / chemical synthesis*
  • Triazoles / therapeutic use
  • Trichophyton / drug effects

Substances

  • Antifungal Agents
  • Triazoles
  • Itraconazole
  • Ketoconazole