Ibrahim Alkhaibari1, Hansa Raj Kc1, Duminduni H Angappulige1, David Gilmore2, Mohammad A Alam1. 1. Department of Chemistry and Physics, College of Science and Mathematics, Arkansas State University, Jonesboro, AR 72467, USA. 2. Department of Biological Sciences, College of Science and Mathematics, Arkansas State University, Jonesboro, AR 72467, USA.
Abstract
Background: Methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci and Acinetobacter baumannii cause serious antibiotic-resistant infections. Finding new antibiotics to treat these infections is imperative for combating this worldwide menace. Methods & Results: 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 S. aureus and Enterococcus faecalis 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. Conclusion: This study demonstrated 20 novel compounds with potent antibacterial activity that are tolerated by human cell lines.
Background: Methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci and Acinetobacter baumannii cause serious antibiotic-resistant infections. Finding new antibiotics to treat these infections is imperative for combating this worldwide menace. Methods & Results: 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 S. aureus and Enterococcus faecalis 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. Conclusion: This study demonstrated 20 novel compounds with potent antibacterial activity that are tolerated by human cell lines.
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Authors: Raj Kc Hansa; M M K Khan; M M Frangie; D F Gilmore; R S Shelton; A V Savenka; A G Basnakian; S L Shuttleworth; M S Smeltzer; M A Alam Journal: Eur J Med Chem Date: 2021-04-04 Impact factor: 7.088
Authors: Pavel A Nazarov; Roman S Kirsanov; Stepan S Denisov; Ljudmila S Khailova; Marina V Karakozova; Konstantin G Lyamzaev; Galina A Korshunova; Konstantin A Lukyanov; Elena A Kotova; Yuri N Antonenko Journal: Biomolecules Date: 2020-02-15
Authors: Rawan Alnufaie; Hansa Raj Kc; Nickolas Alsup; Jedidiah Whitt; Steven Andrew Chambers; David Gilmore; Mohammad A Alam Journal: Molecules Date: 2020-06-15 Impact factor: 4.411