设计并合成抗耐甲氧西林金黄色葡萄球菌的苯并咪唑基苯磺酰胺类化合物。用于预测抗菌活性的定量构效关系研究。

Design and synthesis of anti-MRSA benzimidazolylbenzene-sulfonamides. QSAR studies for prediction of antibacterial activity.

机构信息

Programa de Doctorado en Ciencias Biológicas, Universidad Autónoma Metropolitana, México DF, Mexico.

出版信息

Molecules. 2010 Dec 29;16(1):175-89. doi: 10.3390/molecules16010175.

DOI:10.3390/molecules16010175

PMID:21191320

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6259222/

Abstract

A series of benzimidazolylbenzenesulfonamide compounds containing electron-releasing and electron-withdrawing substituents were synthesized and tested for their in vitro antibacterial activity. Two BZS compounds showed strong antibacterial activity against methicillin-resistant Staphylococcus aureus and Bacillus subtilis. Quantitative studies of their structure-activity relationship using a simple linear regression analysis were applied to explore the correlation between the biological activity and the charges on acidic hydrogen atoms in the synthesized compounds.

摘要

一系列含有供电子和吸电子取代基的苯并咪唑基苯磺酰胺化合物被合成并测试其体外抗菌活性。两种 BZS 化合物对耐甲氧西林金黄色葡萄球菌和枯草芽孢杆菌表现出很强的抗菌活性。采用简单线性回归分析对其构效关系进行定量研究，以探讨合成化合物中酸性氢原子上的电荷与生物活性之间的相关性。