Title:Synthesis and Urease Inhibitory Activity of Some 5-Aminomethylene Barbituric/Thiobarbituric Acid Derivatives
Volume: 15
Issue: 4
Author(s): Mehdi Asadi, Mohammad Mahdavi, Shabnam Mahernia, Zahra Rezaei, Maliheh Safavi, Mina Saeedi and Massoud Amanlou*
Affiliation:
- Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran,Iran
Keywords:
Barbituric acid, thiobarbituric acid, isocyanides, urease inhibitory activity, docking study.
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.