Synthesis,evaluation, and molecular docking studies of aryl urea‐triazole‐based derivatives as anti‐urease agents |
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| Authors: | Setareh Moghimi Fereshteh Goli‐Garmroodi Maryam Allahyari‐Devin Hedieh Pilali Malihe Hassanzadeh Shabnam Mahernia Mohammad Mahdavi Loghman Firoozpour Massoud Amanlou Alireza Foroumadi |
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| Affiliation: | 1. The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran;2. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran;3. Department of Medicinal Chemistry, School of Pharmacy, Urmia University of Medical Science, Urmia, Iran;4. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Research Institute, Tehran University of Medical Sciences, Tehran, Iran;5. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran |
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| Abstract: | 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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| Keywords: | click reaction docking study triazole urease |
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