Novel azole-sulfonamide conjugates as potential antimicrobial candidates : synthesis and biological assessment
Background: Azole and sulfonamide molecular frameworks are endowed with potent antimicrobial activity. Materials & methods: A series of azole-sulfonamide conjugates were synthesized using click reaction of N-propargylated imidazole with azide of sulfonamide and its antimicrobial efficacy was evaluated. Results: The compounds 7c, 7i and 7r displayed promising antibacterial activities, better than the standards sulfonamide and norfloxacin. All molecules exhibited promising antifungal activity, more potent than fluconazole. Docking studies of the active conjugates signified the importance of hydrophobic interactions in hosting the molecules in the active site of dihydrofolate reductase. Conclusion: Azole-sulfonamide conjugates are more active than single sulfonamide moieties and 7c, 7i and 7r may prove valuable leads for further optimization as novel antimicrobial agents.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:16 |
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| Enthalten in: |
Future medicinal chemistry - 16(2024), 2 vom: 11. Jan., Seite 157-171 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Periwal, Pratibha [VerfasserIn] |
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| Links: |
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| Themen: |
21240MF57M |
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| Anmerkungen: |
Date Completed 19.01.2024 Date Revised 19.01.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0251 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM366962302 |
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| 245 | 1 | 0 | |a Novel azole-sulfonamide conjugates as potential antimicrobial candidates |b synthesis and biological assessment |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Background: Azole and sulfonamide molecular frameworks are endowed with potent antimicrobial activity. Materials & methods: A series of azole-sulfonamide conjugates were synthesized using click reaction of N-propargylated imidazole with azide of sulfonamide and its antimicrobial efficacy was evaluated. Results: The compounds 7c, 7i and 7r displayed promising antibacterial activities, better than the standards sulfonamide and norfloxacin. All molecules exhibited promising antifungal activity, more potent than fluconazole. Docking studies of the active conjugates signified the importance of hydrophobic interactions in hosting the molecules in the active site of dihydrofolate reductase. Conclusion: Azole-sulfonamide conjugates are more active than single sulfonamide moieties and 7c, 7i and 7r may prove valuable leads for further optimization as novel antimicrobial agents | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a Kumar, Devinder |e verfasserin |4 aut | |
| 700 | 1 | |a Kumar, Ashwani |e verfasserin |4 aut | |
| 700 | 1 | |a Bhatia, Meenakshi |e verfasserin |4 aut | |
| 700 | 1 | |a Thakur, Sourbh |e verfasserin |4 aut | |
| 700 | 1 | |a Parshad, Mahavir |e verfasserin |4 aut | |
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