Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones.
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.
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis*; D001232:Aspergillus fumigatus / Q000187:drug effects; D002175:Candida / Q000187:drug effects; D002181:Candidiasis, Vulvovaginal / Q000188:drug therapy; D003455:Cryptococcus neoformans / Q000187:drug effects; D003881:Dermatomycoses / Q000188:drug therapy; D005260:Female; D006168:Guinea Pigs; D017964:Itraconazole; D007654:Ketoconazole / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D008864:Microsporum / Q000187:drug effects; D010676:Phialophora / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D013175:Sporothrix / Q000187:drug effects; D014230:Triazoles / Q000138:chemical synthesis* / Q000627:therapeutic use; D014249:Trichophyton / Q000187:drug effects
D000935:Antifungal Agents; D014230:Triazoles; D017964:Itraconazole; D007654:Ketoconazole