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

A Tsuruoka, Y Kaku, H Kakinuma, I TSUKADA…

Index: Tsuruoka, Akihiko; Kaku, Yumiko; Kakinuma, Hiroyuki; Tsukada, Itaru; Yanagisawa, Manabu; Nara, Kazumasa; Naito, Toshihiko Chemical and Pharmaceutical Bulletin, 1998 , vol. 46, # 4 p. 623 - 630

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Citation Number: 32

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 ...