7-Piperazinylquinolones with methylene-bridged nitrofuran scaffold as new antibacterial agents
Abstract Quinolone class of antibacterial agents has considerable attention to find new useful antibacterial agents. Therefore, a series of N-substituted piperazinylquinolones bearing (5-nitrofuran-2-yl)methyl moiety were synthesized and evaluated against a variety of bacteria. The methylene-bridged nitrofuran functionality has been recently used in oxazolidinone class of antibacterial agents containing piperazinyl moiety by introducing ranbezolid as a 5-nitrofuran analog of eperzolid. The results of antibacterial evaluation revealed that the influence of (5-nitrofuran-2-yl) attachment to the 7-piperazinylquinolones against different bacterial species depends on the type of substituents at the N-1 and C-8 positions. Better results were obtained with ethyl at N-1 and CF at C-8 in the term of activity against Bacillus subtilis and E. coli. While, the optimum activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumonia was entailed by a molecule possessing cyclopropyl at N-1 and CH at C-8..
| Medienart: |
Artikel |
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| Erscheinungsjahr: |
2013 |
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| Erschienen: |
2013 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:22 |
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| Enthalten in: |
Medicinal chemistry research - 22(2013), 12 vom: 28. März, Seite 5940-5947 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Emami, Saeed [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| Themen: |
5-Nitrofuran |
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| Anmerkungen: |
© Springer Science+Business Media New York 2013 |
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| doi: |
10.1007/s00044-013-0581-9 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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OLC2049363206 |
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| 520 | |a Abstract Quinolone class of antibacterial agents has considerable attention to find new useful antibacterial agents. Therefore, a series of N-substituted piperazinylquinolones bearing (5-nitrofuran-2-yl)methyl moiety were synthesized and evaluated against a variety of bacteria. The methylene-bridged nitrofuran functionality has been recently used in oxazolidinone class of antibacterial agents containing piperazinyl moiety by introducing ranbezolid as a 5-nitrofuran analog of eperzolid. The results of antibacterial evaluation revealed that the influence of (5-nitrofuran-2-yl) attachment to the 7-piperazinylquinolones against different bacterial species depends on the type of substituents at the N-1 and C-8 positions. Better results were obtained with ethyl at N-1 and CF at C-8 in the term of activity against Bacillus subtilis and E. coli. While, the optimum activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumonia was entailed by a molecule possessing cyclopropyl at N-1 and CH at C-8. | ||
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| 700 | 1 | |a Samadi, Nasrin |4 aut | |
| 700 | 1 | |a Soltani-Ghofrani, Narges |4 aut | |
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