Exploration of (3‐benzyl‐5‐hydroxyphenyl)carbamates as new antibacterial agents against Gram‐positive bacteria,Archiv der Pharmazie

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Exploration of (3‐benzyl‐5‐hydroxyphenyl)carbamates as new antibacterial agents against Gram‐positive bacteria
Archiv der Pharmazie ( IF 4.3 ) Pub Date : 2020-01-02 , DOI: 10.1002/ardp.201900294
Hua-Ju Liang ₁ , Ya-Juan Cheng ₁ , Lu-Xia Wang ₂ , Bao-Qin Huang ₁ , Niu-Niu Zhang ₁ , Jie Liang ₁ , Ming Yan ₁

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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.

中文翻译：

探索（3-苄基-5-羟基苯基）氨基甲酸酯作为抗革兰氏阳性菌的新型抗菌剂

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细菌显示出有效的抑制活性。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产生了深远的影响。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（最低抑制浓度 = 4–8 µg/ml）菌株表现出最有效的抑制活性。初步实验证据表明，这些氨基甲酸酯靶向细菌细胞壁并与万古霉素具有相似的作用机制。

更新日期：2020-01-02

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