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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
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Research Institute, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Biotechnology, Iranian Research Organization for Science and Technology, P. O. Box 3353-5111, Tehran, Iran
  4. 4. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  5. 5. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran

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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