1027280-21-2Relevant academic research and scientific papers
Optically active antifungal azoles. VIII synthesis and antifungal activity of 1-[(1R,2R)-2-(2,4-difluoro- and 2-fluorophenyl)-2-hydroxy-1- methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-3-(4-substituted phenyl)2(1H,3H)- imidazolones and 2-imidazolidinones
Kitazaki, Tomoyuki,Tasaka, Akihiro,Tamura, Norikazu,Matsushita, Yoshihiro,Hosono, Hiroshi,Hayashi, Ryogo,Okonogi, Kenji,Itoh, Katsumi
, p. 351 - 359 (1999)
New optically active antifungal azoles, 1-[(1R,2R)-2-(2,4-difluoro- and 2-fluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-3-(4- substituted phenyl)-2(1H,3H)-imidazolones (1, 2) and 2-imidazolidinones (3, 4), were prepared in a stereocontrolled manner from (1S)-1-[(2R)-2-(2,4- difluoro- and 2-fluorophenyl)-2-oxi-ranyl]ethanols (15, 16). Compounds 1 - 4 showed potent antifungal activity against Candida albicans in vitro and in vivo, as well as a broad antifungal spectrum for various fungi in vitro. Furthermore, the imidazolidinones, 3b - e and 4d, e, were found to exert extremely strong growth-inhibitory activity against Aspergillus fumigatus.
