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Synthesis and Urease Inhibitory Activity of Some 5-Aminomethylene Barbituric/Thiobarbituric Acid Derivatives Publisher



Asadi M1 ; Mahdavi M2 ; Mahernia S1 ; Rezaei Z1 ; Safavi M3 ; Saeedi M4, 5 ; Amanlou M1
Authors

Source: Letters in Drug Design and Discovery Published:2018


Abstract

Background: In this work, a wide spectrum of 5-aminomethylene barbituric/ thiobarbituric acid derivatives was synthesized and evaluated for their Jack bean urease inhibitory activity. 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. © 2018 Bentham Science Publishers.
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