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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.

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cis-β-Methylstyrene is oxidized either with the Fe(III)–H2O2 or with the Fe(II)–O2 complex systems of bleomycin and the synthetic model ligand PYML-6 to give optically active epoxide, showing that the environment around the iron-nucleus is chiral enough to cause asymmetric epoxidation.

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A Novel Route for Chiral Synthesis of the Triazole Antifungal ER-30346. -Starting from the commercially available ester (S)-(I) a novel approach to the key intermediate (XI) for the synthesis of the title compound is developed [last yield is given in gram]. -(KAKU, Y.; TSURUOKA, A.; KAKINUMA, H.; TSUKADA, I.; YANAGISAWA, M.; NAITO, T.; Chem.

Synthesis and Antifungal Activity of Novel Thiazole-Containing Triazole Antifungals.-A series of new thiazole-containing triazole (IV), (X), (XI), and (XII) antifungals is synthesized on a route shown for the derivatives (IV). A detailed structure-activity relationship study is presented to elucidate the influence of constitution and bulkiness of substituents on the antifungal activity. The most promising results are obtained for derivative (IVd). Moreover, an enantioselective synthesis of the more potent (R)-isomer of (IVd) utilizing Sharpless asymmetric dihydroxylation as the key step is given. -(TSURUOKA, A.; KAKU, Y.; KAKINUMA, H.; TSUKADA, I.; YANAGISAWA, M.; NAITO, T.; Chem.