Antifungal activity of conjugated styryl ketones

The susceptibility of Aspergillus fumigatus to a series of alpha, beta-unsaturated styryl ketones known to be thiol-alkylators was examined, and the results were compared with those obtained for Candida albicans. Among 13 compounds used in our study, one (designated NC1110) inhibited the growth of A. fumigatus completely at low concentrations (minimum inhibitory concentration = 32 microM). Structure-activity analysis of these compounds indicated that the electron attracting property as well as the overall hydrophobicity of the compounds are important parameters for their antifungal activity. These preliminary results suggest that further modification of these molecules to enhance their hydrophobicity and the electron attracting property may result in more active compounds with improved antifungal activity.