1. Design, synthesis, and biological evaluation of 4-chloro-2H-thiochromenes featuring nitrogen-containing side chains as potent antifungal agents
- Author
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Dan-Jiao Wang, Xin Su, Zhuang Hou, Hang Xu, Chun Guo, and Ran An
- Subjects
Antifungal ,Antifungal Agents ,Cell Survival ,Nitrogen ,medicine.drug_class ,Clinical Biochemistry ,Pharmaceutical Science ,Microbial Sensitivity Tests ,010402 general chemistry ,01 natural sciences ,Biochemistry ,Cell Line ,Candida tropicalis ,Structure-Activity Relationship ,Drug Discovery ,medicine ,Side chain ,Animals ,Humans ,MTT assay ,Thiamine ,Candida albicans ,Cytotoxicity ,Molecular Biology ,Candida ,Cryptococcus neoformans ,biology ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,biology.organism_classification ,In vitro ,Rats ,0104 chemical sciences ,A549 Cells ,Drug Design ,Molecular Medicine - Abstract
A series of 4-chloro-2H-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-2H-thiochromenes with nitrogen-containing groups provide new lead structures in the search for novel antifungal agents.
- Published
- 2018