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- ISSN: 1570-1808
- E-ISSN: 1875-628X
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Synthesis and Urease Inhibitory Activity of Some 5-Aminomethylene Barbituric/Thiobarbituric Acid Derivatives
- Source: Letters in Drug Design & Discovery, Volume 15, Issue 4, Apr 2018, p. 428 - 436
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- 01 Apr 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.
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