Department of Chemistry and Physics, College of Science and Mathematics, Arkansas State University, Jonesboro, AR 72467, USA.
Department of Biological Sciences, College of Science and Mathematics, Arkansas State University, Jonesboro, AR 72467, USA.
Future Med Chem. 2022 Feb;14(4):233-244. doi: 10.4155/fmc-2021-0140. Epub 2021 Dec 8.
Methicillin-resistant , vancomycin-resistant enterococci and cause serious antibiotic-resistant infections. Finding new antibiotics to treat these infections is imperative for combating this worldwide menace. In this study, the authors designed and synthesized potent antimicrobial agents using 4-trifluoromethylphenyl-substituted pyrazole derivatives. In addition to their potency against planktonic bacteria, potent compounds effectively eradicated and biofilms. Human cells tolerated these compounds with good selectivity factors. Furthermore, the authors provide evidence for the mode of action of compounds based on time-kill kinetics, flow cytometry analysis of propidium iodide-treated bacteria and oxygen uptake studies. This study demonstrated 20 novel compounds with potent antibacterial activity that are tolerated by human cell lines.
耐甲氧西林、万古霉素耐药肠球菌和 导致严重的抗生素耐药感染。寻找新的抗生素来治疗这些感染对于对抗这一全球威胁至关重要。在这项研究中，作者设计并合成了使用 4-三氟甲基苯基取代的吡唑衍生物的有效抗菌剂。除了对浮游细菌的有效性外，有效化合物还能有效清除 和 生物膜。这些化合物对人细胞具有良好的选择性。此外，作者还基于时间杀灭动力学、碘化丙啶处理细菌的流式细胞术分析和耗氧研究提供了化合物作用模式的证据。这项研究展示了 20 种具有强大抗菌活性的新型化合物，这些化合物对人细胞系具有良好的耐受性。
