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Graphical abstract Highlights • Twenty-six 4-chloro-2 H -thiochromenes were designed and synthesized. • Most compounds showed good antifungal activities against tested fungal strains. • Compound 10e and 10y showed better efficacy than fluconazole against strain 103. Abstract A series of 4-chloro-2 H -thiochromenes featuring nitrogen-containing side chains were designed, synthesized and tested in vitro for their antifungal activities. The results of preliminary antifungal tests showed that most target compounds exhibited good inhibitory activities against Candida albicans , Cryptococcus neoformans , Candida tropicalis. Notably, compounds 10e and 10y showed most potent activity in vitro against a variety of fungal pathogens with low MICs. Meanwhile, low cytotoxicity on mammalian cells has been observed for compounds 10e and 10y in the tested concentrations by the MTT assay. Therefore, the 4-chloro-2 H -thiochromenes with nitrogen-containing groups provide new lead structures in the search for novel antifungal agents. [ABSTRACT FROM AUTHOR]