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

Author(s): Mehdi Asadi, Mohammad Mahdavi, Shabnam Mahernia, Zahra Rezaei, Maliheh Safavi, Mina Saeedi, Massoud Amanlou*

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 4 , 2018


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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.

Keywords: Barbituric acid, thiobarbituric acid, isocyanides, urease inhibitory activity, docking study.

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Article Details

VOLUME: 15
ISSUE: 4
Year: 2018
Page: [428 - 436]
Pages: 9
DOI: 10.2174/1570180814666170727142928
Price: $65

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