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

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.

Cite this article as:

Asadi Mehdi , Mahdavi Mohammad , Mahernia Shabnam , Rezaei Zahra , Safavi Maliheh , Saeedi Mina and Amanlou Massoud *, Synthesis and Urease Inhibitory Activity of Some 5-Aminomethylene Barbituric/Thiobarbituric Acid Derivatives, Letters in Drug Design & Discovery 2018; 15 (4) . https://dx.doi.org/10.2174/1570180814666170727142928

DOI https://dx.doi.org/10.2174/1570180814666170727142928	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X