期刊
SCIENTIA PHARMACEUTICA
卷 90, 期 1, 页码 -出版社
MDPI
DOI: 10.3390/scipharm90010002
关键词
fluoroquinolones; ciprofloxacin; norfloxacin; synthesis; antibiotic resistance; molecular docking; antibacterial activity
资金
- Ministry of Health of Ukraine [0121U109239]
The research focuses on synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin, using docking studies and biological activity evaluations to find promising active molecules. A synthetic method was successfully developed, resulting in compounds with enhanced activity compared to the initial molecules, showing great potential.
Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by H-1 NMR,C- 13 NMR, F-19 NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.
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