Abstract
We herein document the discovery of 5-arylidene-2,2-dimethyl-1,3-dioxane-4,6-diones as a novel family of platelet aggregation inhibitors. The preliminary optimization study enabled us to establish the most salient features of the structure-activity relationships in this series as well as to identify novel derivatives that are upto 60 times more potent than the hit structure 1 and slightly superior to the reference drug Milrinone.
Keywords: Antiplatelet agents, Meldrum´s acid, platelet aggregation inhibitors, SAR, 5-Arylidene-2, 2-Dimethyl-1, 3-Dioxane-4, 6-Diones, Milrinone, antithrombotic agents, novel chemotypes, chemical genomics, signal transduction
Combinatorial Chemistry & High Throughput Screening
Title:Discovery and Preliminary SAR of 5-Arylidene-2,2-Dimethyl-1,3-Dioxane- 4,6-Diones as Platelet Aggregation Inhibitors
Volume: 15 Issue: 7
Author(s): Abdelaziz El Maatougui, JhonnyAzuaje, Alberto Coelho, Ernesto Cano, Matilde Yanez, Carmen Lopez, Vicente Yaziji, Carlos Carbajales and Eddy Sotelo
Affiliation:
Keywords: Antiplatelet agents, Meldrum´s acid, platelet aggregation inhibitors, SAR, 5-Arylidene-2, 2-Dimethyl-1, 3-Dioxane-4, 6-Diones, Milrinone, antithrombotic agents, novel chemotypes, chemical genomics, signal transduction
Abstract: We herein document the discovery of 5-arylidene-2,2-dimethyl-1,3-dioxane-4,6-diones as a novel family of platelet aggregation inhibitors. The preliminary optimization study enabled us to establish the most salient features of the structure-activity relationships in this series as well as to identify novel derivatives that are upto 60 times more potent than the hit structure 1 and slightly superior to the reference drug Milrinone.
Export Options
About this article
Cite this article as:
El Maatougui Abdelaziz, JhonnyAzuaje , Coelho Alberto, Cano Ernesto, Yanez Matilde, Lopez Carmen, Yaziji Vicente, Carbajales Carlos and Sotelo Eddy, Discovery and Preliminary SAR of 5-Arylidene-2,2-Dimethyl-1,3-Dioxane- 4,6-Diones as Platelet Aggregation Inhibitors, Combinatorial Chemistry & High Throughput Screening 2012; 15 (7) . https://dx.doi.org/10.2174/138620712801619122
DOI https://dx.doi.org/10.2174/138620712801619122 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...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
-
Combination of Photodynamic Therapy with Anti-Cancer Agents
Current Medicinal Chemistry Emerging Therapies for Type 2 Diabetes
Current Drug Therapy Old and New Gasotransmitters in the Cardiovascular System: Focus on the Role of Nitric Oxide and Hydrogen Sulfide in Endothelial Cells and Cardiomyocytes
Current Pharmaceutical Biotechnology Hypotensive Natural Products: Current Status
Mini-Reviews in Medicinal Chemistry Potentials of Polymeric Nanoparticle as Drug Carrier for Cancer Therapy: With a Special Reference to Pharmacokinetic Parameters
Current Drug Metabolism Proteasome Inhibitors and Modulators of Angiogenesis in Multiple Myeloma
Current Medicinal Chemistry Molecular Dynamics of Protein Kinase-Inhibitor Complexes: A Valid Structural Information
Current Pharmaceutical Design Synthesis and Biological Evaluations of Cytotoxic and Antiangiogenic Triterpenoids-Jacaranone Conjugates
Medicinal Chemistry Towards Isozyme-Selective HDAC Inhibitors For Interrogating Disease
Current Topics in Medicinal Chemistry Cyclodextrins for Non-Viral Gene and siRNA Delivery
Pharmaceutical Nanotechnology New Immunosuppressants in Clinical Trial
Current Drug Targets - Cardiovascular & Hematological Disorders Nitrosative Stress During Infection-Induced Inflammation in Fish: Lessons From a Host-Parasite Infection Model
Current Pharmaceutical Design Myelodysplastic Syndromes: Review of Pathophysiology and Current Novel Treatment Approaches
Current Cancer Drug Targets Reviewing Antiviral Research against Viruses Causing Human Diseases - a Structure-Guided Approach
Current Molecular Pharmacology A Critical Appraisal of the Functional Evolution of P2Y12 Antagonists as Antiplatelet Drugs
Current Pharmaceutical Design Design of multifunctional nanocarriers for delivery of anti-cancer therapy
Current Pharmaceutical Design Chronic Effects of Cocaine on Dopaminergic and Serotonergic Systems of Rats
Current Molecular Imaging (Discontinued) Endothelial Dysfunction in the Hypertensive State: Mechanisms of Hypertensive Cardiovascular Complications
Current Hypertension Reviews Mucosal Delivery of Vaccines: Role of Mucoadhesive/Biodegradable Polymers
Recent Patents on Drug Delivery & Formulation Kinins and Cardiovascular Diseases
Current Pharmaceutical Design