- Semicarbazone derivatives as urease inhibitors: Synthesis, biological evaluation, molecular docking studies and in-silico ADME evaluation
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A series of hydrazinecarboxamide derivatives were synthesized and examined against urease for their inhibitory activity. Among the series, the 1-(3-fluorobenzylidene)semicarbazide (4a) (IC50 = 0.52 ± 0.45 μM), 4u (IC50 = 1.23 ± 0.32 μM) and 4h (IC50 = 2.22 ± 0.32 μM) were found most potent. Furthermore, the molecular docking study was also performed to demonstrate the binding mode of the active hydrazinecarboxamide with the enzyme, urease. In order to estimate drug likeness of compounds, in silico ADME evaluation was carried out. All compounds exhibited favorable ADME profiles with good predicted oral bioavailability.
- Qazi, Syeda Uroos,Rahman, Shafiq Ur,Awan, Asia Naz,al-Rashida, Mariya,Alharthy, Rima D.,Asari, Asnuzilawati,Hameed, Abdul,Iqbal, Jamshed
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- Some aryl semicarbazones possessing anticonvulsant activities
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A number of aryl semicarbazones displayed anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazone (scPTZ) screens when administered intraperitoneally to mice.When given by the oral route to rats, protections was affor
- Dimmock, J. R.,Sidhu, K. K.,Tumber, S. D.,Basran, S. K.,Chen, M.,et al.
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p. 287 - 302
(2007/10/02)
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