Optically Active Antifungal Azoles. II. Synthesis and Antifungal Activity of Polysulfide Derivatives of (2R, 3R)-2-(2,4-Difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl)-2-butanol

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In an effort to find potent antifungal agents, a variety of optically active triazole derivatives with a polysulfide structure, 3,4 and 5,were prepared and evaluated for antifungal activity against Candida albicans in vitro and in vivo. The symmetrical polysulfides 3 (m=2-4) were obtained by an oxidative coupling reaction of (2R, 3R)-2-(2,4-difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl)-2-butanol (1) or by the treatment of its thiocarbonate derivative 8 with potassium tert-butoxide. The unsymmetrical disulfides 5 were synthesized by the reaction of the thiol 1 with Bunte salts 11 or the thiosulfinate 12 or by the reaction of the thiocarbonate 8 with various thiols 13. All of these polysulfides showed potent antifungal activity against candidosis in mice.
公益社団法人日本薬学会の論文
1993-06-15