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
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
Integrating Network Pharmacology and Traditional Medicine: A New Perspective in Drug Mechanism Research
Network pharmacology is a network construction and network topology analysis strategy that combines pharmacology and pharmacodynamics. In recent years, network pharmacology has emerged as a powerful tool that can be integrated with pharmacology. Natural products commonly function in multicomponent, multitarget, and multipathway systems. Some examples encompass Ayurveda, traditional Chinese medicines ...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
-
The Design of Amphiphilic Polymeric Micelles of Curcumin for Cancer Management
Current Medicinal Chemistry Cellobiose Dehydrogenase – A Flavocytochrome from Wood-Degrading, Phytopathogenic and Saprotropic Fungi
Current Protein & Peptide Science Revolutionary Impact of Nanodrug Delivery on Neuroscience
Current Neuropharmacology Identification of New Inhibitors for Human SIRT1: An in-silico Approach
Medicinal Chemistry The Mechanisms of Anticancer Agents by Genistein and Synthetic Derivatives of Isoflavone
Mini-Reviews in Medicinal Chemistry Molecular Imaging with Small Animal PET/CT
Current Medical Imaging Adverse HBOC-Endothelial Dysfunction Synergism: A Possible Contributor to Adverse Clinical Outcomes?
Current Drug Discovery Technologies “Oxygen Supply” as Modulator of Aging Processes: Hypoxia and Hyperoxia Models for Aging Studies
Current Aging Science Hydrogen Sulfide and its Modulation in Arterial Hypertension and Atherosclerosis
Cardiovascular & Hematological Agents in Medicinal Chemistry Moderate Wine Consumption in the Prevention of Metabolic Syndrome and its Related Medical Complications
Endocrine, Metabolic & Immune Disorders - Drug Targets Xanthone Derivatives: New Insights in Biological Activities
Current Medicinal Chemistry Nutritional and Therapeutic Potential of Garlic and Onion (Allium sp.)
Current Nutrition & Food Science The Fundamental Role of Stress Echo in Evaluating Coronary Artery Disease in Specific Patient Populations
Current Vascular Pharmacology Physiology of Folic Acid in Health and Disease
Current Drug Metabolism Nanocrystals as Effective Delivery Systems of Poorly Water-soluble Natural Molecules
Current Medicinal Chemistry Preclinical Evaluation of Coronary Stents: Focus on Safety Issues
Current Vascular Pharmacology The Antimitotic Potential of PARP Inhibitors, An Unexplored Therapeutic Alternative
Current Topics in Medicinal Chemistry Application of MALDI/SELDI Mass Spectrometry to Cancer Biomarker Discovery and Validation
Current Proteomics Development of a Chitosan-based Nanoparticle Formulation for Ophthalmic Delivery of Honokiol
Current Drug Delivery Neuroinflamm-Aging and Neurodegenerative Diseases: An Overview
CNS & Neurological Disorders - Drug Targets