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Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
Eur J Med Chem. 2020 Jun 27; 202:112513.EJ

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.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman, Jordan.Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman, Jordan. Electronic address: gh.suaifan@ju.edu.jo.Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman, Jordan.Department of Biotechnology, Faculty of Applied Sciences, UCSI University, Kuala Lumpur, Malaysia.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32623216

Citation

Mohammed, Aya A M., et al. "Design, Synthesis and Antimicrobial Evaluation of Novel Glycosylated-fluoroquinolones Derivatives." European Journal of Medicinal Chemistry, vol. 202, 2020, p. 112513.
Mohammed AAM, Suaifan GARY, Shehadeh MB, et al. Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives. Eur J Med Chem. 2020;202:112513.
Mohammed, A. A. M., Suaifan, G. A. R. Y., Shehadeh, M. B., & Okechukwu, P. N. (2020). Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives. European Journal of Medicinal Chemistry, 202, 112513. https://doi.org/10.1016/j.ejmech.2020.112513
Mohammed AAM, et al. Design, Synthesis and Antimicrobial Evaluation of Novel Glycosylated-fluoroquinolones Derivatives. Eur J Med Chem. 2020 Jun 27;202:112513. PubMed PMID: 32623216.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives. AU - Mohammed,Aya A M, AU - Suaifan,Ghadeer A R Y, AU - Shehadeh,Mayadah B, AU - Okechukwu,Patrick N, Y1 - 2020/06/27/ PY - 2019/10/16/received PY - 2020/05/11/revised PY - 2020/05/19/accepted PY - 2020/7/6/pubmed PY - 2020/7/6/medline PY - 2020/7/6/entrez KW - Antibacterial KW - Antifungal KW - Ciprofloxacin KW - Glucosamine KW - MTT assay KW - Structure-activity relationship SP - 112513 EP - 112513 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 202 N2 - 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. SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/32623216/Design,_synthesis_and_antimicrobial_evaluation_of_novel_glycosylated-fluoroquinolones_derivatives L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(20)30485-2 DB - PRIME DP - Unbound Medicine ER -
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