Synthesis and Antifungal Activity of a Series of Novel 2-Propen-1-one¹⁾

Abstract

New active antifungal agents containing 1, 1-disubstituted ethylenes (No.1-5), 1, 2-disubstituted ethylenes (No.6-9) and substitued 2-propen-1-one derivatives (No.10-68) with azole compounds were prepared and structure-activity relationships were presented.(Z)-1-(4-Chloropheny1)-3-(2, 4-dichloropheny1)-2-(1H-imidazol-1-y1)-2-propen-1-one hydrochloride (No.21), (Z)-1- (5-chloro-2-thieny1)-3-(4-chloropheny1)-2-(1H-imidazol-1-y1)-2-propen-1-one (No.55) and (Z)-1-(5-chloro-2-thienyl)-3-(2, 4-dichlorophenyl)-2-(1H-imidazol-1-yl)-2-propen-1-one (No.56) displayed potent broad-spectrum activity not only against dermatophytes but also against yeast cells (Candida albicans).