Norfloxacin derivatives as DNA gyrase and urease inhibitors : synthesis, biological evaluation and molecular docking
Background: DNA gyrase and urease enzymes are important targets for the treatment of gastroenteritis, appendicitis, tuberculosis, urinary tract infections and Crohn's disease. Materials & methods: Esterification of norfloxacin was performed to enhance DNA gyrase and urease enzyme inhibition potential. Structure elucidation and chemical characterization were done through spectral (1H NMR, Fourier transform IR, 13C NMR) and carbon, hydrogen, nitrogen and sulfur analysis along with molecular docking. Results & conclusion: The majority of derivatives exhibited significant results but the 3e derivative showed maximum bactericidal, DPPH scavenging (96%), DNA gyrase and urease enzyme inhibitory activity with IC50 of 0.15 ± 0.24 and 1.14 ± 0.11 μM respectively which was further supported by molecular docking studies. So, the active derivatives can serve as a lead compound for the treatment of various pathological conditions.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:15 |
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| Enthalten in: |
Future medicinal chemistry - 15(2023), 23 vom: 24. Dez., Seite 2181-2194 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Awan, Breena [VerfasserIn] |
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| Links: |
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| Themen: |
Anti-Bacterial Agents |
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| Anmerkungen: |
Date Completed 20.12.2023 Date Revised 20.12.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0225 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM36488939X |
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| 245 | 1 | 0 | |a Norfloxacin derivatives as DNA gyrase and urease inhibitors |b synthesis, biological evaluation and molecular docking |
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| 500 | |a Date Revised 20.12.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Background: DNA gyrase and urease enzymes are important targets for the treatment of gastroenteritis, appendicitis, tuberculosis, urinary tract infections and Crohn's disease. Materials & methods: Esterification of norfloxacin was performed to enhance DNA gyrase and urease enzyme inhibition potential. Structure elucidation and chemical characterization were done through spectral (1H NMR, Fourier transform IR, 13C NMR) and carbon, hydrogen, nitrogen and sulfur analysis along with molecular docking. Results & conclusion: The majority of derivatives exhibited significant results but the 3e derivative showed maximum bactericidal, DPPH scavenging (96%), DNA gyrase and urease enzyme inhibitory activity with IC50 of 0.15 ± 0.24 and 1.14 ± 0.11 μM respectively which was further supported by molecular docking studies. So, the active derivatives can serve as a lead compound for the treatment of various pathological conditions | ||
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| 700 | 1 | |a Khan, Mohsin Abbas |e verfasserin |4 aut | |
| 700 | 1 | |a Ahmad, Irshad |e verfasserin |4 aut | |
| 700 | 1 | |a Masood, Anum |e verfasserin |4 aut | |
| 700 | 1 | |a Raza, Asim |e verfasserin |4 aut | |
| 700 | 1 | |a Khaliq, Saharish |e verfasserin |4 aut | |
| 700 | 1 | |a Ullah, Farhat |e verfasserin |4 aut | |
| 700 | 1 | |a Ahmed, Javed |e verfasserin |4 aut | |
| 700 | 1 | |a Khan, Muhammad Rizwan |e verfasserin |4 aut | |
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