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Synthesis and antifungal activity of novel thiazole-containing triazole antifungals. II. Optically active ER-30346
A Tsuruoka1, Y Kaku, H Kakinuma
1Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.
Chemical & Pharmaceutical Bulletin
|May 14, 1998
Abstract:
A series of novel thiazole-containing triazole antifungals was synthesized and evaluated for antifungal activity against a variety of clinically isolated pathogenic fungi in vitro and against systemic candidosis in vivo. These compounds showed potent antifungal activities in vitro and in vivo. In particular, (2R,3R)-3-[4-(4-cyanophenyl)thiazol-2-yl]-2-(2,4- difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (12g; ER-30346) showed potent and well-balanced in vitro activities and potent in vivo efficacy, and had a good safety profile.