Background: In this work, a wide spectrum of 5-aminomethylene barbituric/
thiobarbituric acid derivatives was synthesized and evaluated for their Jack bean urease inhibitory
Methods: Among the synthesized compounds, 5-cyclohexylaminomethylene barbituric acid (3a)
showed the most potent activity (IC50 = 25.8 µM), 4 times more potent than hydroxyurea (IC50 =
100.0 µM) and a similar activity to thiourea (IC50 = 22.0 µM), both being as the reference drugs.
Results and Conclusion: Also, results from docking studies were in good agreement with those
obtained in in vitro assay.