Synthesis and antifungal activity of novel thiazole-containing triazole antifungals. II. Optically active ER-30346 and its derivatives.
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.
Tsuruoka
A
A
Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.
Kaku
Y
Y
Kakinuma
H
H
Tsukada
I
I
Yanagisawa
M
M
Nara
K
K
Naito
T
T
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002177:Candidiasis / Q000188:drug therapy*; D003470:Culture Media; D005658:Fungi / Q000187:drug effects; D051379:Mice; D008826:Microbial Sensitivity Tests; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000935:Antifungal Agents; D003470:Culture Media; D013844:Thiazoles; D014230:Triazoles; C104066:ER 30346