Synthesis and antifungal activity investigation of a novel clotrimazole derivative

Abstract

Azole antifungal agents disrupt fungal ergosterol synthesis that is essential for the formation of fungal cell membrane by preventing 14-α-demethylase enzyme from binding to its substrate. Clotrimazole is one of the first generations of azole antifungal agents. To discover a novel azole antifungal agent, biphenyl derivative was synthesised together with clotrimazole by multistep linear synthesis. Structures of synthesised azole agents have been validated by spectral analysis and potential antifungal activity of both compounds was determined on an yeast, E.coli and M.luteus by using a disk diffusion method. Clotrimazole and its biphenyl derivative were active against yeast but a novel compound resulted less activity than clotrimazole. Antibacterial effect was not observed for either azole agents. DOI: http://dx.doi.org/10.5564/mjc.v14i0.194 Mongolian Journal of Chemistry 14 (40), 2013, p28-32