Synthesis and antifungal activity of new azole derivatives containing an oxathiane ring

A series of azole derivatives containing an oxathiane ring, which were designed to simulate the D ring of lanosterol, were synthesized and evaluated for their antifungal activity. 3,3-Dimethyl derivatives showed potent activity against murine systemic candidosis and aspergillosis, whereas (2R*,3R*)-3-monomethyl derivatives showed only weak activity in both in vitro and in vivo.