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Synthesis, evaluation, and molecular docking studies of aryl urea‐triazole‐based derivatives as anti‐urease agents
Author(s) -
Moghimi Setareh,
GoliGarmroodi Fereshteh,
AllahyariDevin Maryam,
Pilali Hedieh,
Hassanzadeh Malihe,
Mahernia Shabnam,
Mahdavi Mohammad,
Firoozpour Loghman,
Amanlou Massoud,
Foroumadi Alireza
Publication year - 2018
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201800005
Subject(s) - chemistry , urease , docking (animal) , aryl , combinatorial chemistry , urea , triazole , stereochemistry , organic chemistry , medicine , alkyl , nursing
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 IC 50 = 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.