Bioorganic Research Laboratory, Department of Chemistry, University of Allahabad, Allahabad 211002, India.
Bioorganic Research Laboratory, Department of Chemistry, University of Allahabad, Allahabad 211002, India.
Bioorg Med Chem. 2018 Jul 23;26(12):3414-3428. doi: 10.1016/j.bmc.2018.05.015. Epub 2018 May 11.
A new series of heterocyclic molecules bearing sulfonamide linkage has been synthesized and screened for antibacterial activity. During antibacterial screening using broath dilution method, molecules were found to be highly active (MIC value 50-3.1 µg/mL) against different human pathogens, namely B. cerus, S. aureus, E. coli and P. aeruginosa, and most effective against E. coli. A great synergistic effect was observed during determination of FIC where molecules were used in combination with reference drugs chloramphenicol and sulfamethoxazole. The MIC value of the combination - varying concentration of test compounds and ½ MIC of reference drugs or varying concentration of reference drugs and ½ MIC of test compounds, was reduced up to / or / of the original value, indicating thereby the combination was 4-32 times more potent than the test molecule. The molecules also showed low degree of cytotoxicity against PBM, CEM and VERO cell lines. The results positively indicated towards the development of lead antibacterials using the combination approach.
已经合成了一系列带有磺酰胺键的新型杂环分子，并对其进行了抗菌活性筛选。在使用肉汤稀释法进行抗菌筛选时，发现这些分子对不同的人类病原体具有很高的活性（MIC 值为 50-3.1μg/ml），特别是对大肠杆菌有效。在测定 FIC 时观察到了很强的协同作用，其中将这些分子与对照药物氯霉素和磺胺甲恶唑联合使用。组合的 MIC 值（测试化合物的浓度变化与对照药物的 1/2MIC 或对照药物的浓度变化与测试化合物的 1/2MIC）降低了原数值的 / 或 /，这表明该组合的效力比测试分子高 4-32 倍。这些分子对 PBM、CEM 和 VERO 细胞系的细胞毒性也较低。这些结果表明，使用联合方法开发新型抗菌药物具有积极意义。
