化学
恶二唑
脚手架
抗生素
组合化学
立体化学
有机化学
生物化学
程序设计语言
计算机科学
作者
Lyubov Vinogradova,Kristina Komarova,М. В. Чудинов,Elizaveta Rogacheva,Lyudmila Краева,Alexey Lukin
标识
DOI:10.1016/j.mencom.2024.04.016
摘要
Isosteric replacement of the oxadiazole ring by amide bond in the structure of new non-β-lactam antibiotics led to compounds with higher activity against Gram-positive pathogens of ESKAPE panel. A series of 17 compounds were synthesized by acylation of 4-(4-fluorophenoxy)aniline with various amino acids. The spirocyclic derivative with 6-methylsulfonyl-2,6-diazaspiro[3.4]octane moiety showed excellent minimum inhibitory concentrations of 0.093–0.75 μg ml−1 against a number of methicillin-resistant Staphylococcus aureus strains.
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