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

[ Vol. 15 , Issue. 4 ]

Author(s):

Mehdi Asadi, Mohammad Mahdavi, Shabnam Mahernia, Zahra Rezaei, Maliheh Safavi, Mina Saeedi and Massoud Amanlou*   Pages 428 - 436 ( 9 )

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.

Affiliation:

Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Research Institute, Tehran University of Medical Sciences, Tehran, Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Department of Biotechnology, Iranian Research Organization for Science and Technology, Tehran P. O. Box 3353-5111, Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran

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