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

Jan Heeres, L. J. J. Backx, J. Van Cutsem

Journal of Medicinal Chemistry · 1984 · 140 citations · 0 references

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.