Synthesis and antifungal activity of alkylthio and alkylsulfonyl derivatives of SM-8668

Triazole analogues which contained alkylthio or alkylsulfonyl groups where synthesized as derivatives of antifungal SM-8668 and estimated for their in vitro and in vivo activity. Derivatives having pentylthio, heptylthio or nonylthio groups showed excellent efficacy against both candidiasis and aspergillosis. Introduction of a hydrophilic group at the end of their alkyl chain made their activity stronger. Especially, 5-hydroxypentylthio and 7-hydroxyheptylthio derivatives showed the strongest antifungal activity. Alkyl derivatives of sulfur-containing triazoles 1 were synthesized and estimated for their antifungal activities. Some of the compounds showed potent activities against both candidiasis and aspergillosis. The induction of hydroxyl group at the end of their alkyl chain made their activities stronger.