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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

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 and Massoud Amanlou*

Volume 15, Issue 4, 2018

Page: [428 - 436] Pages: 9

DOI: 10.2174/1570180814666170727142928

Price: $65

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.

Graphical Abstract

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