Abstract
In our search for new compounds among the structural analogues of the Picotamide acting on antiplatelet aggregation activities, a new series 2 of 4-ethoxyisophthal-amides were synthesized and their in vitro anti-platelet aggregation activities were evaluated by Born’s test in comparison with their structural analogues of the series 1 of 4-methoxyisophthal-amides. The results revealed, among the series 2, six compounds 200, 2a, 2k, 2n, 2q and 2r displayed good antiplatelet aggregation activities in vitro induced by 5.0 mM ADP with IC50 values ranging over 0.35 μM - 0.77 μM. And of which, compound 2a exhibited the highest in vitro activity superior than two control drugs Picotamide and Aspirin. From a structure-affnity-’Relationship (SAR) pointed of some insight in the view of the role played by 4-ethoxy derivatives.
Keywords: Antiplatelet aggregation, 4-ethoxyisophthalamide, picotamide, synthesis.
Cardiovascular & Hematological Agents in Medicinal Chemistry
Title:Synthesis and the Evaluations in vitro Antiplatelet Aggregation Activities of 4-Ethoxyisophthalamides
Volume: 13 Issue: 2
Author(s): Xiu J. Liu, Tian En Shi, Xiao Wang, Ting T. Wei and Xia Meng
Affiliation:
Keywords: Antiplatelet aggregation, 4-ethoxyisophthalamide, picotamide, synthesis.
Abstract: In our search for new compounds among the structural analogues of the Picotamide acting on antiplatelet aggregation activities, a new series 2 of 4-ethoxyisophthal-amides were synthesized and their in vitro anti-platelet aggregation activities were evaluated by Born’s test in comparison with their structural analogues of the series 1 of 4-methoxyisophthal-amides. The results revealed, among the series 2, six compounds 200, 2a, 2k, 2n, 2q and 2r displayed good antiplatelet aggregation activities in vitro induced by 5.0 mM ADP with IC50 values ranging over 0.35 μM - 0.77 μM. And of which, compound 2a exhibited the highest in vitro activity superior than two control drugs Picotamide and Aspirin. From a structure-affnity-’Relationship (SAR) pointed of some insight in the view of the role played by 4-ethoxy derivatives.
Export Options
About this article
Cite this article as:
Liu J. Xiu, Shi En Tian, Wang Xiao, Wei T. Ting and Meng Xia, Synthesis and the Evaluations in vitro Antiplatelet Aggregation Activities of 4-Ethoxyisophthalamides, Cardiovascular & Hematological Agents in Medicinal Chemistry 2015; 13 (2) . https://dx.doi.org/10.2174/187152571302151217142711
DOI https://dx.doi.org/10.2174/187152571302151217142711 |
Print ISSN 1871-5257 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6182 |
Call for Papers in Thematic Issues
Medicinal Plants with Beneficial Properties on Diabetes and Hypertension
Diabetes and hypertension are real scourges of the 21st century. It is imperative to act in order to find innovative solutions to this problem. Taking medications such as hypoglycemic and antihypertensive drugs may aggravate certain underlying comorbidities, such as chronic kidney disease and cardiovascular disease. This significant drawback therefore requires ...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
-
Traditional and Innovative Anti-seizure Medications Targeting Key Physiopathological
Mechanisms: Focus on Neurodevelopment and Neurodegeneration
Current Neuropharmacology Stable Gastric Pentadecapeptide BPC 157: Prompt Particular Activation of Collateral Pathways
Current Medicinal Chemistry Antiplatelet Agents and Anticoagulants: From Pharmacology to Clinical Practice
Current Pharmaceutical Design Identifying Risk Factors for Clinically Significant Diabetic Macula Edema in Patients with Type 2 Diabetes Mellitus
Current Diabetes Reviews Cell-Penetrating Peptide Technology to Deliver Chaperones and Associated Factors in Diseases and Basic Research
Current Pharmaceutical Biotechnology The Role of 5-HT1A Receptors in Research Strategy for Extensive Pain Treatment
Current Topics in Medicinal Chemistry Properties of the Mesenchymal Endometriotic Stem Cell in the Context of the Immune System and Analysis of its Role in Endometriosis
Recent Patents on Regenerative Medicine Neurotrophin Receptor Signaling as a Therapeutic Target for Huntington's Disease
CNS & Neurological Disorders - Drug Targets Beta-Blockers (Carvedilol) in Children with Systemic Ventricle Systolic Dysfunction - Systematic Review and Meta-Analysis
Reviews on Recent Clinical Trials Developing an Automatic Vision based Abdominal Muscle Extraction and Analysis Method from Ultrasonography
Current Medical Imaging Prediction of Thrombin and Factor Xa Inhibitory Activity with Associative Neural Networks
Current Computer-Aided Drug Design Comparison of the Effects of Contralaterally Controlled Functional Electrical Stimulation and Neuromuscular Electrical Stimulation on Upper Extremity Functions in Patients with Stroke
CNS & Neurological Disorders - Drug Targets Direct Oral Anticoagulants Compared with Vitamin K Antagonists for Left Ventricular Thrombus: A Systematic Review and Meta-analysis
Current Pharmaceutical Design Pharmacological Inhibitors of Cysteinyl Leukotrienes Biosynthesis: Therapeutic Implications
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Intra-arterial Instillation of a Nociceptive Agent Modulates Cardiorespiratory Parameters Involving 5-HT3 and TRPV1 Receptors in Anesthetized Rats
Cardiovascular & Hematological Disorders-Drug Targets Association of Cerebrospinal Fluid Adiponectin Levels With Cerebral Glucose Metabolism In Mild Cognitive Impairment: A Pilot Study
Current Alzheimer Research Polyphenols’ Effect on Cerebrovascular Health
Current Medicinal Chemistry Kinematic and Pressure Features of Handwriting and Drawing: Preliminary Results Between Patients with Mild Cognitive Impairment, Alzheimer Disease and Healthy Controls
Current Alzheimer Research Asymmetric Dimethylarginine: a Key Player in the Pathophysiology of Endothelial Dysfunction, Vascular Inflammation and Atherosclerosis in Rheumatoid Arthritis?
Current Pharmaceutical Design Applications of Positron Emission Tomography in Neuropsychiatric Pharmaceutical Drug Development
Current Radiopharmaceuticals