Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 74, Issue -, Pages 314-323Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.01.001
Keywords
Thiourea derivatives; Synthesis; In vitro urease inhibition activity; Kinetic study
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Funding
- Organization for Prohibition of Chemical Weapons (OPCW), The Netherlands
- Higher Education Commission (HEC) Pakistan [L/ICA/ICB/173681/12, 20-1910]
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Thiourea derivatives (1-38) were synthesized and evaluated for their urease inhibition potential. The synthetic compounds showed a varying degree of in vitro urease inhibition with IC50 values 5.53 +/- 0.02 -91.50 +/- 0.08 mu M, most of which are superior to the standard thiourea (IC(5)0 = 21.00 +/- 0.11 mu M). In order to ensure the mode of inhibition of these compounds, the kinetic study of the most active compounds has been carried out. Most of these inhibitors were found to be mixed-type of inhibitors, except compounds 13 and 30 which were competitive, while compound 19 was identified as non-competitive inhibitor with Ki values between 8.6 and 19.29 mu M. (C) 2014 Elsevier Masson SAS. All rights reserved.
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