Abstract

Therapeutic options for preventing the trajectory of multi-drug resistance bacterial pathogens could rely on the effort to design a novel technique to develop a potent antimicrobial agent to counter the key issue. To curb the current outbreak, we synthesized first generation of antimicrobial amine-modified carbon quantum dots, CQDs–NH₂ as carbon precursors followed by hydrothermal carbonization of ethylenediamine/citric acid, and postmodified with propargyl alcohol (CQDs-1) and quinoline derivative; 8-hydroxy quinoline (CQDs-2) through Cu(I)-catalyzed azide-alkyne cycloaddition. The novel clicked 1,2,3-triazole functionalized CQDs–NH₂ templates, were evaluated against standard Gram-positive; Staphylococcus aureus (S. aureus), and Gram-negative; Escherichia coli (E. coli), MRSA, along with clinical-resistant diabetic foot PUS swab isolated bacterial pathogens by 96-well method as well as agar-well diffusion method, to unleased the potential antibacterial activity. 1,2,3-triazole functionalized CQDs–NH₂ template showed enhanced antibacterial activity against distinct bacterial strains, with minimum inhibitory concentration for standard bacteria, MRSA-bacteria, and clinical resistant bacterial pathogens in the range of 0.25–8, 64–128, and 128–256 μg mL⁻¹ respectively. This nanobiotic template displays good potential through the hybridization of 1,2,3-triazole with antibacterial pharmacophores CQDs–NH₂ and quinoline, to overcome drug resistance, reduce toxicity, and improve pharmacokinetic profiles. The findings of this study might have a favorable impact on antibiotic pharmacodynamics and, as a result, nanobiotic dosing regimens as well as clinical outcomes.

Graphical Abstract

中文翻译：

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利用喹啉基三唑功能化碳量子点通过点击化学对抗临床耐药细菌病原体的纳米生物制剂

摘要

防止多重耐药细菌病原体发展的治疗选择可能依赖于设计一种新技术来开发有效的抗菌剂来解决这个关键问题。为了遏制当前的疫情，我们合成了第一代抗菌胺修饰碳量子点，CQDs–NH ₂作为碳前体，然后进行乙二胺/柠檬酸的水热碳化，并用炔丙醇（CQDs-1）和喹啉衍生物进行后修饰；通过 Cu(I) 催化的叠氮化物-炔环加成反应生成 8-羟基喹啉 (CQDs-2)。新型点击 1,2,3-三唑功能化 CQDs-NH ₂模板，针对标准革兰氏阳性菌进行了评估；金黄色葡萄球菌（S. aureus）和革兰氏阴性；大肠杆菌( E. coli )、MRSA以及临床耐药的糖尿病足PUS拭子通过96孔法和琼脂孔扩散法分离出细菌病原体，以释放潜在的抗菌活性。 1,2,3-三唑功能化的CQDs–NH ₂模板对不同的细菌菌株表现出增强的抗菌活性，对标准细菌、MRSA细菌和临床耐药细菌病原体的最低抑菌浓度在0.25–8、64–128范围内，和 128–256 μg mL ^-1分别。这种纳米生物模板通过 1,2,3-三唑与抗菌药效团 CQDs-NH ₂和喹啉的杂交显示出良好的潜力，可以克服耐药性、降低毒性并改善药代动力学特征。这项研究的结果可能对抗生素药效学产生有利影响，从而对纳米抗生素给药方案以及临床结果产生有利影响。

图形概要