Anti-Candida Activity of 4-Morpholino-5-Nitro- and 4,5-Dinitro-Imidazole Derivatives

Abstract

The activities of some 4-morpholino-5-nitro- and 4,5-dinitro-imidazole derivatives with respect to several Candida species were evaluated. It is established that 4,5-dinitroimidazole derivatives constitute an important group of compounds possessing antifungal activity against Candida species. Some analogs showed moderate antifungal ability in vitro, especially in relation well-known antifungals such as flucytosine (5FC). The best results of antifungal action were obtained for 1-(3-bromo-2-hydroxypropyl)-2-methyl-4,5-dinitroimidazole (3c), 1-(3-bromo-2-oxopropyl)-2-methyl-4,5-dinitroimidazole (4c) and 2-methyl-1-phenacyl-4,5-dinitroimidazole (2b). The latter compound proved to be effective against Candida sake S-1 (in contrast to inactive 5FC).