Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Synthesis and Antifungal Activity of Novel Thiazole-Containing Triazole Antifungals. II. Optically Active ER-30346 and Its Derivatives
Akihiko TSURUOKAYumiko KAKUHiroyuki KAKINUMAItaru TSUKADAManabu YANAGISAWAKazumasa NARAToshihiko NAITO
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1998 Volume 46 Issue 4 Pages 623-630

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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 vitro activities and potent in vivo efficacy, and had a good safety profile.

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© The Pharmaceutical Society of Japan
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