The Search for New Antibacterial Agents among 1,2,3-Triazole Functionalized Ciprofloxacin and Norfloxacin Hybrids: Synthesis, Docking Studies, and Biological Activity Evaluation

被引:19
作者
Hryhoriv, Halyna [1 ]
Mariutsa, Illia [2 ]
Kovalenko, Sergiy M. [3 ]
Georgiyants, Victoriya [1 ]
Perekhoda, Lina [4 ]
Filimonova, Nataliia [5 ]
Geyderikh, Olga [5 ]
Sidorenko, Lyudmila [1 ]
机构
[1] Natl Univ Pharm, Pharmaceut Chem Dept, UA-61153 Kharkiv, Ukraine
[2] Natl Univ Pharm, Organ Chem Dept, UA-61153 Kharkiv, Ukraine
[3] Kharkov Natl Univ, Organ Chem Dept, UA-61022 Kharkiv, Ukraine
[4] Natl Univ Pharm, Med Chem Dept, UA-61153 Kharkiv, Ukraine
[5] Natl Univ Pharm, Virol & Immunol, Dept Microbiol, UA-61153 Kharkiv, Ukraine
关键词
fluoroquinolones; ciprofloxacin; norfloxacin; synthesis; antibiotic resistance; molecular docking; antibacterial activity; MOLECULAR DOCKING; DERIVATIVES;
D O I
10.3390/scipharm90010002
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
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页数:20
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