Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent

J Med Chem. 1979 Aug;22(8):1003-5. doi: 10.1021/jm00194a023.

Abstract

The preparation and antifungal properties of cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl-methyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazine (I) are described. Ketoconazole has, at low oral doses, a high in vivi activity against vaginal candidosis in rats and against cutaneous candidosis in guinea pigs.

MeSH terms

  • Animals
  • Antifungal Agents / chemical synthesis*
  • Candidiasis / drug therapy
  • Chemical Phenomena
  • Chemistry
  • Female
  • Guinea Pigs
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use
  • Miconazole / therapeutic use
  • Piperazines / chemical synthesis*
  • Piperazines / pharmacology
  • Rats

Substances

  • Antifungal Agents
  • Imidazoles
  • Piperazines
  • Miconazole