OPTICALLY-ACTIVE ANTIFUNGAL AZOLES .3. SYNTHESIS AND ANTIFUNGAL ACTIVITY OF SULFIDE AND SULFONAMIDE DERIVATIVES OF YL)-3-MERCAPTO-1-(1H-1,2,4-TRIAZOL-1-YL)-2-BUTANOL

In an effort to find potent antifungal agents, optically active sulfur -containing triazole derivatives, sulfides (3) and sulfonamides (4), w ere prepared and evaluated for antifungal activity against Candida alb icans in vitro and in vivo. The sulfides (3) were prepared by the reac tion of yl)-3-mercapto-1-(1H-1,2,4-triazol-l-yl)-2-butanol (1) with va rious heteroaryhnethyl chlorides in the presence of sodium methoxide. The sulfonamides (4) were synthesized starting from the disulfide (15) in three steps including oxidation of the corresponding sulfenamides (17). Some of the sulfur-containing triazole derivatives (3, 4) showed strong protective effects against candidosis in mice.