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探索(3-苄基-5-羟基苯基)氨基甲酸酯类化合物作为新型抗革兰氏阳性菌的抗菌药物。

Exploration of (3-benzyl-5-hydroxyphenyl)carbamates as new antibacterial agents against Gram-positive bacteria.

机构信息

Guangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China.

Department of Clinical Laboratory, Guangzhou Liuhuaqiao Hospital, Guangzhou, China.

出版信息

Arch Pharm (Weinheim). 2020 Mar;353(3):e1900294. doi: 10.1002/ardp.201900294. Epub 2020 Jan 2.

Abstract

A series of (3-benzyl-5-hydroxyphenyl)carbamates were evaluated as new antibacterial agents. Several compounds showed potent inhibitory activity against sensitive and drug-resistant Gram-positive bacteria. The compounds are ineffective against all tested Gram-negative bacteria. The structure of the ester group exerted a profound effect on antibacterial activity. 4,4-Dimethylcyclohexanyl carbamate 6h exhibited the most potent inhibitory activity against the standard and clinically isolated Staphylococcus aureus, Staphylococcus epidermidis, and Enterococcus faecalis (minimum inhibitory concentration = 4-8 µg/ml) strains. The preliminary experimental evidence indicated that these carbamates target the bacterial cell wall and share a similar mechanism of action with vancomycin.

摘要

一系列(3-苄基-5-羟基苯基)氨基甲酸酯被评估为新型抗菌剂。几种化合物对敏感和耐药的革兰氏阳性菌表现出很强的抑制活性。这些化合物对所有测试的革兰氏阴性菌均无效。酯基的结构对抗菌活性有深远的影响。4,4-二甲基环己基氨基甲酸酯 6h 对标准和临床分离的金黄色葡萄球菌、表皮葡萄球菌和粪肠球菌(最小抑菌浓度 = 4-8μg/ml)菌株表现出最强的抑制活性。初步的实验证据表明,这些氨基甲酸酯类药物的作用靶点是细菌细胞壁,与万古霉素的作用机制相似。

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