Journal
BIOORGANIC CHEMISTRY
Volume 82, Issue -, Pages 163-177Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.09.036
Keywords
In vitro urease inhibitory activity; Benzohydrazide; In silico studies; Kinetic studies
Funding
- Higher Education Commission (HEC) Pakistan [20-1910, D/14/520]
- Organization for the Prohibition of Chemical Weapons (OPCW), The Hague, The Netherlands [D/14/520]
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Benzohydrazide derivatives 1-43 were synthesized via one-pot reaction and structural characterization of these synthetic derivatives was carried out by different spectroscopic techniques such as H-1 NMR and EI-MS. The synthetic molecules were evaluated for their in vitro urease inhibitory activity. All synthetic derivatives showed good inhibitory activities in the range of (IC50 = 0.87 +/- 0.31-19.0 +/- 0.25 mu M) as compared to the standard thiourea (IC50 = 21.25 +/- 0.15 mu M), except seven compounds 17, 18, 23, 24, 29, 30, and 41 which were found to be inactive. The most active compound of the series was compound 36 (IC50 = 0.87 +/- 0.31 mu M) having two chloro groups at meta positions of ring A and methoxy group at para position of ring B. The structure-activity relationship (SAR) of the active compounds was established on the basis of different substituents and their positions in the molecules. Kinetic studies of the active compounds revealed that compounds can inhibit enzyme via competitive and noncompetitive modes. In silico study was also performed to understand the binding interactions of the molecules (ligand) with the active site of enzyme.
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