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.
Letters in Drug Design & Discovery
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.
Export Options
About this article
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Co-administration of Saffron and Chamomile Give Additive Effects of
Antidiabetic and Antioxidant Activity with <i>In vivo</i> Augmentation of Brain
BDNF, Acetylcholine Levels and Cognitive Functions in Streptozotocininduced
Diabetic Rats
Current Psychopharmacology Adiponectin and its Role in Cardiovascular Diseases
Cardiovascular & Hematological Disorders-Drug Targets Therapeutic Angiogenesis by Gene Therapy for Critical Limb Ischemia: Choice of Biological Agent
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) D-Galactose as a Vector for Prodrug Design
Current Topics in Medicinal Chemistry Pre-B Cell Colony Enhancing Factor/NAMPT/Visfatin in Inflammation and Obesity- Related Disorders
Current Pharmaceutical Design The Chemistry and Pharmacology of Genistein
The Natural Products Journal Serine Protease Inhibitor Kazal Type 1 (SPINK1): Beyond the Trypsin Inhibitor
Current Enzyme Inhibition Survivin as a Prognostic/Predictive Marker and Molecular Target in Cancer Therapy
Current Medicinal Chemistry The Role of Target Therapy in the Treatment of Gastrointestinal Noncolorectal Cancers: Clinical Impact and Cost Consideration
Current Cancer Drug Targets Molecular and Cellular Regulators of Cancer Angiogenesis
Current Cancer Drug Targets Therapeutics Interventions with Anti-Inflammatory Creams in Post Radiation Acute Skin Reactions: A Systematic Review of Most Important Clinical Trials
Recent Patents on Inflammation & Allergy Drug Discovery Chemotherapy and Delivery in the Treatment of Primary Brain Tumors
Current Clinical Pharmacology Lipids as Delivery Systems to Improve the Biological Activity of Bioactive Ingredients
Current Nutrition & Food Science Antipsoriatic Drug Development: Challenges and New Emerging Therapies
Recent Patents on Inflammation & Allergy Drug Discovery Oxidative Stress and its Clinical Consequences: Relationship between Diabetes and Cancer
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Critical Functions of lncRNA DGCR5 in Cancers of the Digestive System
Current Pharmaceutical Design Non-Analgesic Effects of Opioids: Management of Opioid-Induced Constipation by Peripheral Opioid Receptor Antagonists: Prevention or Withdrawal?
Current Pharmaceutical Design Preformulation Designed to Enable Discovery and Assess Developability
Combinatorial Chemistry & High Throughput Screening Bioactivity of Sesquiterpenes: Compounds that Protect from Alcohol-Induced Gastric Mucosal Lesions and Oxidative Damage
Mini-Reviews in Medicinal Chemistry Novel and Emerging Targeted Therapies of Colorectal Cancer
Current Clinical Pharmacology