Synthesis and antifungal activity of novel thiazole-containing triazole antifungals. II. Optically active ER-30346 and its derivatives

DOI: 10.1248/cpb.46.623

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Chemical and Pharmaceutical Bulletin p. 623 - 630 (1998)

Update date:2022-09-26

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Authors:

Tsuruoka, Akihiko

Kaku, Yumiko

Kakinuma, Hiroyuki

Tsukada, Itaru

Yanagisawa, Manabu

Nara, Kazumasa

Naito, Toshihiko

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Article abstract of DOI:10.1248/cpb.46.623

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-l-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.

Full text of DOI:10.1248/cpb.46.623

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