Chemical and Pharmaceutical Bulletin p. 623 - 630 (1998)
Update date:2022-09-26
Topics:
Tsuruoka, Akihiko
Kaku, Yumiko
Kakinuma, Hiroyuki
Tsukada, Itaru
Yanagisawa, Manabu
Nara, Kazumasa
Naito, Toshihiko
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.
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