金黄色葡萄球菌
DNA旋转酶
大肠杆菌
苯甲酰胺
抗菌活性
化学
二氢蕨酸合酶
化脓性链球菌
立体化学
结合
体外
对接(动物)
微生物学
细菌
生物
生物化学
医学
护理部
数学分析
基因
数学
免疫学
乙胺嘧啶
疟疾
恶性疟原虫
遗传学
作者
Monalisa Mahapatra,Sudhir Kumar Paidesetty,Ajit Kumar Bishoyi,Rabindra N. Padhy
标识
DOI:10.1080/14786419.2021.2022662
摘要
A series of N-heteroaryl substituted Gallamide derivatives 3a-3g were synthesised and the obtained structures were further confirmed by different spectral studies. For in-vitro antibacterial activity, the synthesised compounds were evaluated against three UTI (Urinary Tract Infection) bacterial strains including Staphylococcus aureus, Escherichia coli, and Streptococcus pyogenes. Furthermore, the designed compounds were docked with bacterial DNA gyrase and dihydropteroate synthase. All the compounds had shown good inhibition against S. aureus whereas compound 3e has produced significant inhibition at 28 and 26 mm against S.aureus and E.coli, respectively. The MIC value of the conjugate 3e and 3d was 3.12 and 6.25 μg/mL against S. aureus andE.coli, respectively. Compound 3,4,5-trihydroxy-N-(4-(N-(5-methyl isoxazol-3-yl) sulfamoyl) phenyl)benzamide 3d had shown the highest binding energy against both the targets along with good antibacterial action.
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