![conference banner](/images/conference-banner.jpeg)
Abstract
A series of novel pyrazole carboxylic acid derivatives was designed and synthesized, and their antagonism effect on endothelin (ET)-1-induced contraction in the rat thoracic aortic ring was screened. The radio receptor assay was used to examine the potency of the compounds on ET receptor. Some target compounds demonstrated significant inhibitory activity, especially 7m, which showed a potent inhibition percentage higher than the contrast compound BQ123. Further assays on the binding and selectivity for ET showed that 7m had highly potent binding activity on ETA at the nanomole level, and the ratio of ETA/ETB was 36. Therefore, we inferred that 7m was a non-selective antagonist of ETA and ETB and had potential for further development in cardiovascular diseases.
Keywords: Pyrazole acid, endothelin, antagonist, synthesis, BQ123, cardiovascular.
Medicinal Chemistry
Title:Design, Synthesis, and Bioactivity of Pyrazole Acid Derivatives as Endothelin Receptor Antagonists
Volume: 9 Issue: 8
Author(s): Jin Cai, Ligang Liu, Junqing Chen, Meng Cao and Min Ji
Affiliation:
Keywords: Pyrazole acid, endothelin, antagonist, synthesis, BQ123, cardiovascular.
Abstract: A series of novel pyrazole carboxylic acid derivatives was designed and synthesized, and their antagonism effect on endothelin (ET)-1-induced contraction in the rat thoracic aortic ring was screened. The radio receptor assay was used to examine the potency of the compounds on ET receptor. Some target compounds demonstrated significant inhibitory activity, especially 7m, which showed a potent inhibition percentage higher than the contrast compound BQ123. Further assays on the binding and selectivity for ET showed that 7m had highly potent binding activity on ETA at the nanomole level, and the ratio of ETA/ETB was 36. Therefore, we inferred that 7m was a non-selective antagonist of ETA and ETB and had potential for further development in cardiovascular diseases.
Export Options
About this article
Cite this article as:
Cai Jin, Liu Ligang, Chen Junqing, Cao Meng and Ji Min, Design, Synthesis, and Bioactivity of Pyrazole Acid Derivatives as Endothelin Receptor Antagonists, Medicinal Chemistry 2013; 9 (8) . https://dx.doi.org/10.2174/1573406411309080013
DOI https://dx.doi.org/10.2174/1573406411309080013 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
![Wayfinder Image](/images/wayfinder.jpg)
- 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
-
Alzheimer Biomarkers and Clinical Alzheimer Disease were Not Associated with Increased Cerebrovascular Disease in a Memory Clinic Population
Current Alzheimer Research Proteomics Analysis Revealed an Altered Left Ventricle Protein Profile in a Mouse Model of Transverse Aortic Constriction
Protein & Peptide Letters Beneficial Effects of Azuki Bean (Vigna angularis) Extract: Anti-Oxidant, Anti-Hypertension, and Treatment for Renal Damage
Current Nutrition & Food Science The Role of Renin Angiotensin System Blockade in the Treatment of Atrial Fibrillation
Current Drug Targets - Cardiovascular & Hematological Disorders Preface [Hot topic: Anti-Hypertensive Agents in Relation to Modifying Coronary Risk Factors (Executive Editor : Aurelio Leone)]
Current Pharmaceutical Design Estimation of Familial Combined Hyperlipoproteinemia Prevalence in a Large Rural Population: The Brisighella Heart Study
Vascular Disease Prevention (Discontinued) The Atherosclerotic Plaque Vulnerability: Focus on the Oxidative and Endoplasmic Reticulum Stress in Orchestrating the Macrophage Apoptosis in the Formation of the Necrotic Core
Current Medicinal Chemistry Pisosterol Induces G2/M Cell Cycle Arrest and Apoptosis via the ATM/ATR Signaling Pathway in Human Glioma Cells
Anti-Cancer Agents in Medicinal Chemistry Myocardial Energy Substrate Metabolism in Heart Failure : from Pathways to Therapeutic Targets
Current Pharmaceutical Design Balaglitazone: A Second Generation Peroxisome Proliferator-Activated Receptor (PPAR) Gamma (γ) Agonist
Mini-Reviews in Medicinal Chemistry The Sour Taste-Modifying Protein (Miraculin), Tyrosinase Inhibitors and Antioxidants from Synsepalum dulcificum
Current Nutrition & Food Science The Secondary Heart Field: Understanding Conotruncal Defects from a Developmental Perspective
Current Cardiology Reviews CXCR4-CXCL12-Dependent Inflammatory Network and Endothelial Progenitors
Current Medicinal Chemistry Large Artery Stiffness and Antihypertensive Agents
Current Pharmaceutical Design Thiopurine S-Methyltransferase as a Pharmacogenetic Biomarker: Significance of Testing and Review of Major Methods
Cardiovascular & Hematological Agents in Medicinal Chemistry The Influence of Genetic Variations and Drug Interactions Based on Metabolism of Antidepressants and Anticonvulsants
Current Drug Metabolism Recent Patents and Patent Applications Relating to mTOR Pathway
Recent Patents on DNA & Gene Sequences Vascular Calcification in Chronic Kidney Disease: Role of Disordered Mineral Metabolism
Current Pharmaceutical Design Repurposing of Chemotherapeutics to Combat COVID-19
Current Topics in Medicinal Chemistry Microscopies at the Nanoscale for Nano-Scale Drug Delivery Systems
Current Drug Targets