Saifi Zohaib, Ali Asghar, Inam Afreen, Azam Amir, Kamthan Mohan, Abid Mohammad, Ali Imran
Department of Chemistry, Jamia Millia Islamia Jamia Nagar New Delhi-110025 India
Department of Biosciences, Jamia Millia Islamia New Delhi-110025 India
RSC Adv. 2025 Jan 17;15(3):1680-1689. doi: 10.1039/d4ra05069j. eCollection 2025 Jan 16.
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.
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。