Abstract
Pain and inflammation are simultaneous responses in bacterial infections. In current clinical practice, two groups of agents like antibacterial and non-steroidal anti-inflammatory drugs (NSAIDs) are prescribed simultaneously. Regrettably, none of the drug possesses these activities in a single component. Exploiting the bioisosterism concept, we have documented that 2-phenyl-3-substituted quinazolines, 2,3-disubstituted quinazolines, 2-methyl-3-substituted quinazolin- 4-(3H)-ones and 2-methylthio-3-substituted quinazolin-4-(3H)-ones exhibited good analgesic and anti-inflammatory activities. The present work is an extension of our ongoing efforts towards the development and identification of lead molecules by bioisostere concept, for which we designed some of 2-methylthio-3-substituted-5,6-dimethylthieno[2,3-d] pyrimidin-4(3H)-ones. The title compounds were investigated for analgesic, anti-inflammatory and antibacterial activities. While the test compounds exhibited significant activity, the compounds (6-9) showed more potent analgesic activity, and the compounds (8, 9) showed anti-inflammatory activity comparable to the reference standard diclofenac.
Keywords: Bioisosterism, thienopyrimidine, analgesic, anti-inflammatory
Medicinal Chemistry
Title: Design and Synthesis of 2-Methylthio-3-substituted-5,6-dimethylthieno [2,3-d] pyrimidin-4(3H)-ones as Analgesic, Anti-Inflammatory and Antibacterial Agents
Volume: 3 Issue: 1
Author(s): V. Alagarsamy, V. Raja Solomon, R. Meenac, K. V. Ramaseshu, K. Thirumurugan and S. Murugesan
Affiliation:
Keywords: Bioisosterism, thienopyrimidine, analgesic, anti-inflammatory
Abstract: Pain and inflammation are simultaneous responses in bacterial infections. In current clinical practice, two groups of agents like antibacterial and non-steroidal anti-inflammatory drugs (NSAIDs) are prescribed simultaneously. Regrettably, none of the drug possesses these activities in a single component. Exploiting the bioisosterism concept, we have documented that 2-phenyl-3-substituted quinazolines, 2,3-disubstituted quinazolines, 2-methyl-3-substituted quinazolin- 4-(3H)-ones and 2-methylthio-3-substituted quinazolin-4-(3H)-ones exhibited good analgesic and anti-inflammatory activities. The present work is an extension of our ongoing efforts towards the development and identification of lead molecules by bioisostere concept, for which we designed some of 2-methylthio-3-substituted-5,6-dimethylthieno[2,3-d] pyrimidin-4(3H)-ones. The title compounds were investigated for analgesic, anti-inflammatory and antibacterial activities. While the test compounds exhibited significant activity, the compounds (6-9) showed more potent analgesic activity, and the compounds (8, 9) showed anti-inflammatory activity comparable to the reference standard diclofenac.
Export Options
About this article
Cite this article as:
Alagarsamy V., Raja Solomon V., Meenac R., Ramaseshu V. K., Thirumurugan K. and Murugesan S., Design and Synthesis of 2-Methylthio-3-substituted-5,6-dimethylthieno [2,3-d] pyrimidin-4(3H)-ones as Analgesic, Anti-Inflammatory and Antibacterial Agents, Medicinal Chemistry 2007; 3 (1) . https://dx.doi.org/10.2174/157340607779317599
DOI https://dx.doi.org/10.2174/157340607779317599 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
- 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
-
Association of Mean Platelet Volume with Hypertension in Rheumatoid Arthritis
Inflammation & Allergy - Drug Targets (Discontinued) Modulatory Effects and Molecular Mechanisms of Olive Oil and Other Dietary Lipids in Breast Cancer
Current Pharmaceutical Design Cardiovascular Toxicities with Chimeric Antigen Receptor T-cell Therapy
Current Cardiology Reviews A Novel Class of Emerging Anticancer Compounds: Oxyprenylated Secondary Metabolites from Plants and Fungi
Current Medicinal Chemistry Structure-Editing of Nucleic Acids for Selective Targeting of RNA
Current Topics in Medicinal Chemistry Natural Steroids and Androgen Antagonists used as Neuroprotection in Common Neurological Disorders
CNS & Neurological Disorders - Drug Targets Preface
Current Pharmaceutical Design Protein Oxidation and Proteolytic Signalling in Aging
Current Pharmaceutical Design Experimental Approaches Towards Allergic Asthma Therapy-Murine Asthma Models
Recent Patents on Inflammation & Allergy Drug Discovery Brain Protection and Cognitive Function: Cocoa Flavonoids as Nutraceuticals
Current Pharmaceutical Design In Vivo Monitoring of Cell Based Therapy in the Liver
Current Molecular Imaging (Discontinued) COVID-19 and Inflammatory Markers
Current Vascular Pharmacology Toxicology of Tributyltin in Mammalian Animal Models
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Antinociceptive Activities of Some 4,5-Dihydro-1H-Pyrazole Derivatives: Involvement of Central and Peripheral Pathways
Letters in Drug Design & Discovery Compounds Derived from Epigallocatechin-3-Gallate (EGCG) as a Novel Approach to the Prevention of Viral Infections
Inflammation & Allergy - Drug Targets (Discontinued) Clinical Manifestations, Diagnosis, and Treatment of Endometriosis
Current Women`s Health Reviews Kinase CK2 Inhibition: An Update
Current Medicinal Chemistry A Systems Biology Consideration of the Vasculopathy of Sickle Cell Anemia: The Need for Multi-Modality Chemo-Prophylaxis
Cardiovascular & Hematological Disorders-Drug Targets Editorial (Thematic Issue: Ceramics, Nanotubes, Advanced Materials: Theoretical and Experimental Structure-Property Relationships Part IV)
Current Physical Chemistry The Effects of Placental Corticotrophin Releasing Hormone on the Physiology and Psychology of the Pregnant Woman
Current Women`s Health Reviews