Optically Active Antifungal Azoles. X. Synthesis and Antifungal Activity of N-[4-(Azolyl) phenyl]-and N-[4-(Azolylmethyl) phenyl]-N'-[(1R, 2R)-2-(2, 4-difluorophenyl)-2- …

…, Y MATSUSHITA, R HAYASHI, K OKONOGI…

Index: Kitazaki, Tomoyuki; Ichikawa, Takashi; Tasaka, Akihiro; Hosono, Hiroshi; Matsushita, Yoshihiro; Hayashi, Ryogo; Okonogi, Kenji; Itoh, Katsumi Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 12 p. 1935 - 1946

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Citation Number: 26

Abstract

New optically active antifungal azoles, N-[4-(azolyl) phenyl]-and N-[4-(azolylmethyl) phenyl]- N'-[(1R, 2R)-2-(2, 4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1, 2, 4-triazol-1-yl) propyl] azolones (1, 2, 3), were prepared in a stereocontrolled manner. Compounds 1-3 showed strong antifungal activity against Candida albicans in vitro. Among them, the imidazolidinones 3 showed a broad antifungal spectrum in vitro as well as potent in vivo ...