期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 202, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112513
关键词
Glucosamine; Ciprofloxacin; Antibacterial; Antifungal; MTT assay; Structure-activity relationship
资金
- Deanship of Scientific Research at The University of Jordan (Amman, Jordan) [2213]
Herein we report the design, synthesis and biological evaluation of structurally modified ciprofloxacin, norfloxacin and moxifloxacin standard drugs, featuring amide functional groups at C-3 of the fluoroquinolone scaffold. In vitro antimicrobial testing against various Gram-positive bacteria, Gram-negative bacteria and fungi revealed potential antibacterial and antifungal activity. Hybrid compounds 9 (MIC 0.2668 +/- 0.0001 mM), 10 (MIC 0.1358 +/- 00025 mM) and 13 (MIC 0.0898 +/- 0.0014 mM) had potential antimicrobial activity against a fluoroquinolone-resistant Escherichia coli clinical isolate, compared to ciprofloxacin (MIC 0.5098 +/- 0.0024 mM) and norfloxacin (MIC 0.2937 +/- 0.0021 mM) standard drugs. Interestingly, compound 10 also exerted potential antifungal activity against Candida albicans (MIC 0.0056 +/- 0.0014 mM) and Penicillium chrysogenum (MIC 0.0453 +/- 0.0156 mM). Novel derivatives and standard fluoroquinolone drugs exhibited near-identical cytotoxicity levels against L6 muscle cell-line, when measured using the MIT assay. (C) 2020 Elsevier Masson SAS. All rights reserved.
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