Spiro[benzoxazine-piperidin]-one derivatives as chitin synthase inhibitors and antifungal agents: Design, synthesis and biological evaluation

Autor:	Yajie, Xu, Yangli, Shen, Chuanbiao, Du, Lige, Liu, Hu, Wu, Qingggang, Ji
Rok vydání:	2022
Předmět:	Chitin Synthase Pharmacology Structure-Activity Relationship Antifungal Agents Candida albicans Organic Chemistry Drug Discovery Chitin Microbial Sensitivity Tests General Medicine Enzyme Inhibitors Fluconazole Benzoxazines
Zdroj:	European Journal of Medicinal Chemistry. 243:114723
ISSN:	0223-5234
DOI:	10.1016/j.ejmech.2022.114723
Popis:	Four series of spiro[benzoxazine-piperidin]-one derivatives were designed and synthesized. Their inhibition percentages against chitin synthase and antifungal activities were evaluated. Based on the preliminary biological assays, the series of derivatives containing α, β-unsaturated carbonyl fragment which had moderate to excellent CHS inhibitory activity and antifungal activity were further researched. In this series of compounds, eight out of twenty-one compounds had good to excellent inhibitory activity against chitin synthase with an inhibition percentage value above 60% at the concentration of 300 μg/mL. Among them, compounds 9a, 9o, 9s and 9t showed excellent chitin synthase inhibitory activity with IC
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ebac08922282281f7fe6dcd7c248d30c https://doi.org/10.1016/j.ejmech.2022.114723 Zobrazit plný text záznamu Full Text from ScienceDirect