Design, synthesis, and biological evaluation of 4-chloro-2 H -thiochromenes featuring nitrogen-containing side chains as potent antifungal agents

摘要

A series of 4-chloro-2H-thiochromenes featuring nitrogen-containing side chains were designed, synthesized and testedin vitrofor their antifungal activities. The results of preliminary antifungal tests showed that most target compounds exhibited good inhibitory activities againstCandida albicans,Cryptococcus neoformans,Candida tropicalis. Notably, compounds10eand10yshowed most potent activityin vitroagainst a variety of fungal pathogens with low MICs. Meanwhile, low cytotoxicity on mammalian cells has been observed for compounds10eand10yin the tested concentrations by the MTT assay. Therefore, the 4-chloro-2H-thiochromenes with nitrogen-containing groups provide new lead structures in the search for novel antifungal agents.