2. Academic Validation
  3. Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives

Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives

  • Eur J Med Chem. 2020 Sep 15:202:112513. doi: 10.1016/j.ejmech.2020.112513.
Aya A M Mohammed 1,  Ghadeer A R Y Suaifan 2,  Mayadah B Shehadeh 1,  Patrick N Okechukwu 3
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman, Jordan.
  • 2 Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman, Jordan. Electronic address: gh.suaifan@ju.edu.jo.
  • 3 Department of Biotechnology, Faculty of Applied Sciences, UCSI University, Kuala Lumpur, Malaysia.
PMID: 32623216 DOI: 10.1016/j.ejmech.2020.112513
Abstract

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 MTT assay.

Keywords

Antibacterial; Antifungal; Ciprofloxacin; Glucosamine; MTT assay; Structure-activity relationship.

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