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喹啉-磺酰胺杂化化合物的合成与抗菌评价:一种对抗细菌耐药性的有前景的策略。

Synthesis and antibacterial evaluation of quinoline-sulfonamide hybrid compounds: a promising strategy against bacterial resistance.

作者信息

Saifi Zohaib, Ali Asghar, Inam Afreen, Azam Amir, Kamthan Mohan, Abid Mohammad, Ali Imran

机构信息

Department of Chemistry, Jamia Millia Islamia Jamia Nagar New Delhi-110025 India

Department of Biosciences, Jamia Millia Islamia New Delhi-110025 India

出版信息

RSC Adv. 2025 Jan 17;15(3):1680-1689. doi: 10.1039/d4ra05069j. eCollection 2025 Jan 16.

Abstract

Antibiotic-resistant bacteria are a serious global health threat, making infections harder to treat and increasing medical costs and mortality rates. To combat resistant bacterial strains, a series of compounds (QS1-12) were synthesized with an excellent yield of 85-92%. Initial assessments of these analogues as potential antibacterial agents were conducted through a preliminary screening against a panel of diverse bacterial strains. The results identified compound QS-3 as the most effective antibacterial candidate, exhibiting exceptional inhibitory activity against with a minimum inhibitory concentration (MIC) of 64 μg mL. Furthermore, QS-3 demonstrated a favorable synergistic effect when combined with ciprofloxacin. Notably, the compound displayed minimal cytotoxicity, inducing less than 5% lysis of red blood cells (RBCs). Significantly, QS-3 exhibited enhanced inhibitory activity, particularly against the antibiotic-resistant strains AA202 and AA290. predictions of physicochemical properties underscored the drug-like qualities of the designed compounds. Additionally, molecular docking poses, ligPlot images, and a binding affinity of -8.0 kcal mol further reinforced their potential as promising antibacterial agents. Briefly, the reported compound QS3 may be a future broad-range antibacterial agent.

摘要

抗生素耐药细菌是全球严重的健康威胁,使感染更难治疗,并增加医疗成本和死亡率。为了对抗耐药菌株,合成了一系列化合物(QS1 - 12),产率高达85 - 92%。通过对一组不同细菌菌株的初步筛选,对这些类似物作为潜在抗菌剂进行了初步评估。结果确定化合物QS - 3为最有效的抗菌候选物,对其最小抑菌浓度(MIC)为64μg/mL,表现出卓越的抑制活性。此外,QS - 3与环丙沙星联合使用时表现出良好的协同效应。值得注意的是,该化合物显示出最小的细胞毒性,诱导红细胞(RBC)裂解率低于5%。重要的是,QS - 3表现出增强的抑制活性,特别是对耐药菌株AA202和AA290。物理化学性质预测强调了所设计化合物的类药特性。此外,分子对接姿势、ligPlot图像以及 - 8.0 kcal/mol的结合亲和力进一步增强了它们作为有前景的抗菌剂的潜力。简而言之,所报道的化合物QS3可能是未来的一种广谱抗菌剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f692/11740869/ab663bdbd71f/d4ra05069j-f1.jpg

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