Chemical and Pharmaceutical Bulletin p. 1169 - 1176 (1997)
Update date:2022-09-26
Topics:
Tsuruoka, Akihiko
Kaku, Yumiko
Kakinuma, Hiroyuki
Tsukada, Itaru
Yanagisawa, Manabu
Naito, Toshihiko
A new series of 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. Among these compounds, (±)-1-(2,4-difluorophenyl)-1-[4-(2,4- difluorophenyl)thiazol-2-yl]-2-(1H-1,2,4-triazol-1-yl)ethanol (ER24161) showed the most potent and well-balanced in vitro activities and excellent in vivo efficacy. We also achieved an enantioselective synthesis of the more potent enantiomer of ER-24161.
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