Mehta S, Kumar P, Marwaha R K, Narasimhan B
Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, India.
Drug Res (Stuttg). 2014 Apr;64(4):208-13. doi: 10.1055/s-0033-1355355. Epub 2013 Nov 20.
In the present study, 2-chlorobenzoic acid derivatives were synthesized and evaluated for their antimicrobial activity against Gram-positive bacteria: Staphylococcus aureus, Bascillus subtilis, Gram-negative bacterium Escherichia coli, fungal strains: Candida albicans and Aspergillus niger by tube dilution method. Results of antimicrobial screening indicated that the synthesized compounds exhibited greater antibacterial potential against Gram-negative bacterium (Escherichia coli) than Gram-positive bacteria and the Schiff's bases of 2-chloro benzoic acid were more potent antimicrobial agents than its esters. Compound 6 (pMIC(am)=1.91 µM/ml, pMIC(ec)=2.27 µM/ml) emerged as most potent antimicrobial agent and was found comparable to standard drug norfloxacin (pMIC(ec)=2.61 µM/ml) against Escherichia coli. QSAR studies revealed that the antibacterial, antifungal and the overall antimicrobial activities of the 2-chlorobenzoic acid derivatives were governed by the topological parameters, second order and valence second order molecular connectivity indices ((2)χ and (2)χ(v)).
在本研究中，通过试管稀释法合成了2-氯苯甲酸衍生物，并评估了它们对革兰氏阳性菌（金黄色葡萄球菌、枯草芽孢杆菌）、革兰氏阴性菌（大肠杆菌）以及真菌菌株（白色念珠菌和黑曲霉）的抗菌活性。抗菌筛选结果表明，合成的化合物对革兰氏阴性菌（大肠杆菌）显示出比革兰氏阳性菌更强的抗菌潜力，并且2-氯苯甲酸的席夫碱比其酯类是更有效的抗菌剂。化合物6（对金黄色葡萄球菌的pMIC(am)=1.91 µM/ml，对大肠杆菌的pMIC(ec)=2.27 µM/ml）成为最有效的抗菌剂，并且发现其对大肠杆菌的活性与标准药物诺氟沙星（对大肠杆菌的pMIC(ec)=2.61 µM/ml）相当。定量构效关系（QSAR）研究表明，2-氯苯甲酸衍生物的抗菌、抗真菌及整体抗菌活性受拓扑参数、二阶和价态二阶分子连接性指数（(2)χ和(2)χ(v)）的控制。
