Abstract
In an attempt to find a new class of anti-inflammatory agents, a series of novel benzamides 3 (ab1-ab16) was synthesized by utilizing some arylideneoxazolones 2(az1-az4) having 2-acetyloxyphenyl substitution on their second position. IR, 1H-NMR, 13C NMR and HRMS, confirmed the structures of these synthesized compounds. Among the tested benzamide compounds 3ab1, 3ab2, 3ab11 and 3ab16 showed promising anti-inflammatory activity with lessened propensity to cause gastro-intestinal hypermotility and ulceration when compared with standard Indomethacin. Virtual screening was performed by docking the designed compounds into the ATP binding site of COX-2 receptor to predict if these compounds have analogous binding mode to the COX-2 inhibitor.
Keywords: Anti-inflammatory, benzamides, docking, gastro-intestinal hypermotility, ulcerogenic activity.
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Title:Rational Design and Synthesis of Benzamides as Non-ulcerogenic Anti-inflammatory Agents
Volume: 13 Issue: 3
Author(s): Saurabh Khadse, Vinod Ugale and Gokul Talele
Affiliation:
Keywords: Anti-inflammatory, benzamides, docking, gastro-intestinal hypermotility, ulcerogenic activity.
Abstract: In an attempt to find a new class of anti-inflammatory agents, a series of novel benzamides 3 (ab1-ab16) was synthesized by utilizing some arylideneoxazolones 2(az1-az4) having 2-acetyloxyphenyl substitution on their second position. IR, 1H-NMR, 13C NMR and HRMS, confirmed the structures of these synthesized compounds. Among the tested benzamide compounds 3ab1, 3ab2, 3ab11 and 3ab16 showed promising anti-inflammatory activity with lessened propensity to cause gastro-intestinal hypermotility and ulceration when compared with standard Indomethacin. Virtual screening was performed by docking the designed compounds into the ATP binding site of COX-2 receptor to predict if these compounds have analogous binding mode to the COX-2 inhibitor.
Export Options
About this article
Cite this article as:
Khadse Saurabh, Ugale Vinod and Talele Gokul, Rational Design and Synthesis of Benzamides as Non-ulcerogenic Anti-inflammatory Agents, Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 2014; 13 (3) . https://dx.doi.org/10.2174/1871523013666141017102257
DOI https://dx.doi.org/10.2174/1871523013666141017102257 |
Print ISSN 1871-5230 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-614X |
- 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
-
New Advances in the Molecular Mechanisms Driving Biliary Fibrosis and Emerging Molecular Targets
Current Drug Targets Mesalazine Activates Adenosine Monophosphate-activated Protein Kinase: Implication in the Anti-inflammatory Activity of this Anti-colitic Drug
Current Molecular Pharmacology An Overview of Notch Signaling in Adult Tissue Renewal and Maintenance
Current Alzheimer Research Monocyte Dependent Regulation of Autoimmune Inflammation
Current Molecular Medicine Possible Mechanisms of Lymphoma Development in Sjogren’s Syndrome
Current Immunology Reviews (Discontinued) A Vector Based on the Chicken Hypersensitive Site 4 Insulator Element Replicates Episomally in Mammalian Cells
Current Gene Therapy Biological and Clinical Significance of Endotoxemia in the Course of Hepatitis C Virus Infection
Current Pharmaceutical Design Novel Interpenetrating Polymer Matrix Network Microparticles for Intestinal Drug Delivery
Current Drug Delivery Editorial (Thematic Issue: Vascular Damage In Systemic Sclerosis)
Current Rheumatology Reviews Obesity Related Kidney Disease
Current Diabetes Reviews Preconditioning and Shear Stress in the Microcirculation in Ischemia-Reperfusion Injury
Current Cardiology Reviews Scientific and Clinical Challenges in Sepsis
Current Pharmaceutical Design Multiple Hormonal Dysregulation as Determinant of Low Physical Performance and Mobility in Older Persons
Current Pharmaceutical Design Low Molecular Weight Heparins as Antineoplastic Agents
Recent Patents on Anti-Cancer Drug Discovery Susceptibility Risk Alleles of -238G/A, -308G/A and -1031T/C Promoter Polymorphisms of TNF-α Gene to Uterine Leiomyomas
Recent Advances in DNA & Gene Sequences (Discontinued) Nanocarriers as Tools in Delivering Active Compounds for Immune System Related Pathologies
Recent Patents on Nanotechnology Pathophysiology of Patent Ductus Arteriosus in the Preterm Infant
Current Pediatric Reviews Induction of Myocardial Fibrosis and Hypertrophy by Natriuretic Peptides
Vascular Disease Prevention (Discontinued) Palmitoylethanolamide Regulates Production of Pro-Angiogenic Mediators in a Model of β Amyloid-Induced Astrogliosis <i>In Vitro</i>
CNS & Neurological Disorders - Drug Targets A Novel Treatment Strategy for Sepsis and Septic Shock Based on the Interactions between Prostanoids, Nitric Oxide, and 20-Hydroxyeicosatetraenoic Acid
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry