Synthesis and evaluation of novel antifungal agents targeted to the plasma membrane H[+]-ATPase

Abstract

A library of dienones were synthesized as candidate antifungal agents. These compounds were screened against Saccharomyces cerevisiae and Candida albicans using macro-broth susceptibility assay. The dienones exhibited a broad range of inhibition against S. cerevisiae (0.2-99%) and C. albicans (0-99%). 3,5-bis(p- trifluoromethylbenzylidene)-1-methyl-piperidine-4-one was identified as the most potent inhibitor of S. cerevisiae. Whereas, the most promising inhibitor of C. albicans was 2,6-bis(pyridine-3ylmethylene)cyclohexan-1-one.

Keywords

• n-methylpiperidin-4-one
• dienone
• plasma membrane h+- atpase
• antifungal