Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent.
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.
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis*; D002177:Candidiasis / Q000188:drug therapy; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D006168:Guinea Pigs; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D008825:Miconazole / Q000627:therapeutic use; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000935:Antifungal Agents; D007093:Imidazoles; D010879:Piperazines; D008825:Miconazole