Study on the substituents' effects of a series of synthetic chalcones against the yeast Candida albicans

A large series of chalcones were synthesized and studied for activity against Candida albicans. The SAR analysis showed that the antifungal activity was highly dependent on the substitution pattern of the aryl rings and correlated to a large extent with the ability of compounds to interact with sulfhydryl groups. The most active were the hydroxylated chalcones as their activity related to the location of the phenolic group in the aryl ring B as follows: o-OH > p-OH ∼ 3,4-di-OH > m-OH. These and other correlations obtained strongly contribute to the knowledge for design of anticandidal chalcones.

Amongst a series of compounds the most potent against Candida albicans was the chalcone with n = 0, m = 1, R3′ = R4′ = R5′ = R3 = R4 = R5 = H and R2 = OH.Figure optionsDownload as PowerPoint slide