Synthesis, evaluation, and molecular docking studies of aryl urea-triazole-based derivatives as anti-urease agents
© 2018 Deutsche Pharmazeutische Gesellschaft..
Considering the importance of urease inhibitors in the treatment of ureolytic bacterial infections, in this work, the synthesis of novel, aryl urea-triazole-based derivatives as effective urease inhibitors is described. Dichloro-substituted derivative 4o, with IC50 = 22.81 ± 0.05 μM, is found to be the most potent urease inhibitor, determined by Berthelot colorimetric assay. Docking studies were also carried out for compound 4o to confirm the effective interactions with the urease active site.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2018 |
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| Erschienen: |
2018 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:351 |
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| Enthalten in: |
Archiv der Pharmazie - 351(2018), 7 vom: 24. Juli, Seite e1800005 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Moghimi, Setareh [VerfasserIn] |
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| Links: |
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| Themen: |
8W8T17847W |
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| Anmerkungen: |
Date Completed 19.10.2018 Date Revised 19.10.2018 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1002/ardp.201800005 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM284432288 |
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| 520 | |a © 2018 Deutsche Pharmazeutische Gesellschaft. | ||
| 520 | |a Considering the importance of urease inhibitors in the treatment of ureolytic bacterial infections, in this work, the synthesis of novel, aryl urea-triazole-based derivatives as effective urease inhibitors is described. Dichloro-substituted derivative 4o, with IC50 = 22.81 ± 0.05 μM, is found to be the most potent urease inhibitor, determined by Berthelot colorimetric assay. Docking studies were also carried out for compound 4o to confirm the effective interactions with the urease active site | ||
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