Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro
Quinolones are among the prominent class of broad-spectrum antibiotics. In this work, a series of 1,4-dihydro-4-oxo-3-[3-{benzenesulfon}-2-hydrazino-1-oxo-]quinoline derivatives 6a-e were synthesized and tested for their antibacterial efficacy in vitro. Compounds 6a-e were characterized by NMR (1H,1...
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| Format: | Article |
| Language: | English |
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Elsevier
2022-01-01
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| Series: | Results in Chemistry |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211715622001163 |
| _version_ | 1811198984297906176 |
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| author | Nishtha Saxena Rakesh Kumar Swapnil Shankhdhar Nivedita Srivastava |
| author_facet | Nishtha Saxena Rakesh Kumar Swapnil Shankhdhar Nivedita Srivastava |
| author_sort | Nishtha Saxena |
| collection | DOAJ |
| description | Quinolones are among the prominent class of broad-spectrum antibiotics. In this work, a series of 1,4-dihydro-4-oxo-3-[3-{benzenesulfon}-2-hydrazino-1-oxo-]quinoline derivatives 6a-e were synthesized and tested for their antibacterial efficacy in vitro. Compounds 6a-e were characterized by NMR (1H,13C), HRMS and IR analysis. All these compounds confirmed bactericidal activity against tested bacterial strains. The MIC data have shown that compounds 6e (MIC = 7.5 mg/mL) displayed better activity against Staphylococcus aureus, Escherichia coli (ETEC) and Pseudomonas aeruginosa. Compounds 6b-e (MIC = 7.5 mg/mL) have similar activity as Norfloxacin against E. coli. Molecular docking studies was also conducted to explore binding interactions of our compounds at the active sites of the GyrB subunit of E. coli K-12. |
| first_indexed | 2024-04-12T01:40:19Z |
| format | Article |
| id | doaj.art-1f206a137f1e40f2a68fa6bfa58bc532 |
| institution | Directory Open Access Journal |
| issn | 2211-7156 |
| language | English |
| last_indexed | 2024-04-12T01:40:19Z |
| publishDate | 2022-01-01 |
| publisher | Elsevier |
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| series | Results in Chemistry |
| spelling | doaj.art-1f206a137f1e40f2a68fa6bfa58bc5322022-12-22T03:53:12ZengElsevierResults in Chemistry2211-71562022-01-014100397Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitroNishtha Saxena0Rakesh Kumar1Swapnil Shankhdhar2Nivedita Srivastava3Bio-organic and Heterocyclic Chemistry Research Laboratory, Department of Applied Chemistry, M. J. P. Rohilkhand University, Bareilly-243006, Uttar Pradesh, IndiaBio-organic and Heterocyclic Chemistry Research Laboratory, Department of Applied Chemistry, M. J. P. Rohilkhand University, Bareilly-243006, Uttar Pradesh, IndiaBio-organic and Heterocyclic Chemistry Research Laboratory, Department of Applied Chemistry, M. J. P. Rohilkhand University, Bareilly-243006, Uttar Pradesh, IndiaCorresponding author.; Bio-organic and Heterocyclic Chemistry Research Laboratory, Department of Applied Chemistry, M. J. P. Rohilkhand University, Bareilly-243006, Uttar Pradesh, IndiaQuinolones are among the prominent class of broad-spectrum antibiotics. In this work, a series of 1,4-dihydro-4-oxo-3-[3-{benzenesulfon}-2-hydrazino-1-oxo-]quinoline derivatives 6a-e were synthesized and tested for their antibacterial efficacy in vitro. Compounds 6a-e were characterized by NMR (1H,13C), HRMS and IR analysis. All these compounds confirmed bactericidal activity against tested bacterial strains. The MIC data have shown that compounds 6e (MIC = 7.5 mg/mL) displayed better activity against Staphylococcus aureus, Escherichia coli (ETEC) and Pseudomonas aeruginosa. Compounds 6b-e (MIC = 7.5 mg/mL) have similar activity as Norfloxacin against E. coli. Molecular docking studies was also conducted to explore binding interactions of our compounds at the active sites of the GyrB subunit of E. coli K-12.http://www.sciencedirect.com/science/article/pii/S2211715622001163QuinolonesHydrazineBenzene sulfonyl chlorideMolecular Docking |
| spellingShingle | Nishtha Saxena Rakesh Kumar Swapnil Shankhdhar Nivedita Srivastava Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro Results in Chemistry Quinolones Hydrazine Benzene sulfonyl chloride Molecular Docking |
| title | Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro |
| title_full | Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro |
| title_fullStr | Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro |
| title_full_unstemmed | Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro |
| title_short | Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro |
| title_sort | synthesis of new 3 substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro |
| topic | Quinolones Hydrazine Benzene sulfonyl chloride Molecular Docking |
| url | http://www.sciencedirect.com/science/article/pii/S2211715622001163 |
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