Abstract
The carboxamide derivatives of Febuxostat were synthesized via the reaction of Febuxostat with various amines through by Schotten-Baumann reaction. All the synthesized compounds have been evaluated for their in vitro Xanthine Oxidase inhibitory activity. The present study reveals that most of carboxamides were acting as better XO inhibitors and play an important role in decreasing uricacid levels. Almost all the compounds surprisingly showed nearly 30% higher XO inhibition activities than the standard Allopurinol. 3h, 3k and 3l stand as the best among the synthesized compounds.
Keywords: Febuxostat carboxamide derivatives, Schotten-Baumann reaction, Xanthine oxidase (XO) inhibitory activity.
Letters in Drug Design & Discovery
Title:Augmenting the Xanthine Oxidase Inhibitory Activity of Febuxostat by its Structural Modification
Volume: 11 Issue: 2
Author(s): Kuruva Chandra Sekhar, Golla Madhava, Katla Venkata Ramana, CH. Rama Murthy and Chamarthi Naga Raju
Affiliation:
Keywords: Febuxostat carboxamide derivatives, Schotten-Baumann reaction, Xanthine oxidase (XO) inhibitory activity.
Abstract: The carboxamide derivatives of Febuxostat were synthesized via the reaction of Febuxostat with various amines through by Schotten-Baumann reaction. All the synthesized compounds have been evaluated for their in vitro Xanthine Oxidase inhibitory activity. The present study reveals that most of carboxamides were acting as better XO inhibitors and play an important role in decreasing uricacid levels. Almost all the compounds surprisingly showed nearly 30% higher XO inhibition activities than the standard Allopurinol. 3h, 3k and 3l stand as the best among the synthesized compounds.
Export Options
About this article
Cite this article as:
Chandra Sekhar Kuruva, Madhava Golla, Venkata Ramana Katla, Rama Murthy CH. and Naga Raju Chamarthi, Augmenting the Xanthine Oxidase Inhibitory Activity of Febuxostat by its Structural Modification, Letters in Drug Design & Discovery 2014; 11 (2) . https://dx.doi.org/10.2174/15701808113109990056
DOI https://dx.doi.org/10.2174/15701808113109990056 |
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
-
Targeting Angiogenesis in the Treatment of Multiple
Current Angiogenesis (Discontinued) Biodistribution, Safety and Organ Toxicity of Docetaxel-Loaded in HER-2 Aptamer Conjugated Ecoflex® Nanoparticles in a Mouse Xenograft Model of Ovarian Cancer
Recent Patents on Nanotechnology Differentiation of Pluripotent Stem Cells into Nucleus Pulposus Progenitor Cells for Intervertebral Disc Regeneration
Current Stem Cell Research & Therapy Recent Drug Targets Associated to Abnormal Signal Transduction Mediated Cancer, Rheumatoid Arthritis, Alzheimer’s and Parkinson’s disease
Current Signal Transduction Therapy The Marine Factor 3,5-dihydroxy-4-methoxybenzyl Alcohol Suppresses Cell Growth, Inflammatory Cytokine Production, and NF-κB Signaling-enhanced Osteoclastogenesis in In vitro Mouse Macrophages RAW264.7 Cells
Current Molecular Medicine Study of Prolactin Permeation Through the Pericardium and Its Bioavailability
Protein & Peptide Letters The Importance of mir-491-5p in Various Cancers
Current Molecular Medicine Inhibition of sPLA2-IIA, C-reactive Protein or Complement: New Therapy for Patients with Acute Myocardial Infarction?
Cardiovascular & Hematological Disorders-Drug Targets Preface [HotTopic: Cytokine Therapies for Diabetic Microvascular Complications (Executive Editor: J.L. Wilkinson-Berka)]
Current Pharmaceutical Design Abnormal Insulin Signaling: Early Detection of Silent Coronary Artery Disease-Erectile Dysfunction?
Current Pharmaceutical Design In silico Designing and Screening of Lead Compounds to NS5-Methyltransferase of Dengue Viruses
Medicinal Chemistry A Perspective on Water Site Prediction Methods for Structure Based Drug Design
Current Topics in Medicinal Chemistry A Review of Chinese Herbal Medicine for the Treatment of Chronic Heart Failure
Current Pharmaceutical Design The Discovery of VLA-4 Antagonists
Current Topics in Medicinal Chemistry Biologically Active Peptides Interacting with the G Protein-Coupled Formylpeptide Receptors
Protein & Peptide Letters Streptozotocin-Induced Diabetes Mellitus in Neonatal Rats: An Insight into its Applications to Induce Diabetic Complications
Current Diabetes Reviews What Comparative Genomics Tells Us About the Evolution of Eukaryotic Genes Involved in Recombination
Current Genomics Critical Role of NFκB in the Pathogenesis of Non-alcoholic Fatty Liver Disease: A Widespread Key Regulator
Current Molecular Medicine Cerebellum, GABA and Ataxia
Current Psychopharmacology Integration of Virtual Screening into the Drug Discovery Process
Mini-Reviews in Medicinal Chemistry