Abstract
In the present study we describe the synthesis of a new series of 1,2,4-triazoles: [3-(arylmethyl)thio-5-aryl-4H- [1,2,4]triazol-4-yl]acetic acids 5a-g, [5-(arylmethyl)thio-3-aryl-1H-[1,2,4]triazol-1-yl]acetic acids 8a-d, and [3-(arylmethyl) thio-5-aryl-1H-[1,2,4]triazol-1-yl] acetic acids 9a-d. These compounds were tested in binding assays to evaluate their ability as ligands for human ETA and ETB receptors stably expressed in CHO cells; some of the tested compounds showed affinity in the micromolar range.
Keywords: Hypertension, endothelins, ET receptors, binding assays, 1,2,4-triazoles, regioisomers
Medicinal Chemistry
Title: Synthesis of 1,2,4-triazole Derivatives: Binding Properties on Endothelin Receptors
Volume: 3 Issue: 6
Author(s): L. Salerno, F. Guerrera, M. Modica, G. Romeo, V. Pittala, M. A. Siracusa, I. Mereghetti, A. Cagnotto and T. Mennini
Affiliation:
Keywords: Hypertension, endothelins, ET receptors, binding assays, 1,2,4-triazoles, regioisomers
Abstract: In the present study we describe the synthesis of a new series of 1,2,4-triazoles: [3-(arylmethyl)thio-5-aryl-4H- [1,2,4]triazol-4-yl]acetic acids 5a-g, [5-(arylmethyl)thio-3-aryl-1H-[1,2,4]triazol-1-yl]acetic acids 8a-d, and [3-(arylmethyl) thio-5-aryl-1H-[1,2,4]triazol-1-yl] acetic acids 9a-d. These compounds were tested in binding assays to evaluate their ability as ligands for human ETA and ETB receptors stably expressed in CHO cells; some of the tested compounds showed affinity in the micromolar range.
Export Options
About this article
Cite this article as:
Salerno L., Guerrera F., Modica M., Romeo G., Pittala V., Siracusa A. M., Mereghetti I., Cagnotto A. and Mennini T., Synthesis of 1,2,4-triazole Derivatives: Binding Properties on Endothelin Receptors, Medicinal Chemistry 2007; 3 (6) . https://dx.doi.org/10.2174/157340607782360281
DOI https://dx.doi.org/10.2174/157340607782360281 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
- 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
-
Evaluation of the Risk/Benefit Ratio of Old and New Anti-Inflammatory Drugs
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Melatonin in the Biliary Tract and Liver: Health Implications
Current Pharmaceutical Design Recent Advances in Targeted Anti-Vasculature Therapy: The Neuroblastoma Model
Current Drug Targets Putative Role for Apelin in Pressure/Volume Homeostasis and Cardiovascular Disease
Cardiovascular & Hematological Agents in Medicinal Chemistry Pharmacologic Role of Vitamin D Natural Products
Current Vascular Pharmacology Characterization and Management of Cutaneous Side Effects Related to the Immunosuppressive Treatment in Solid Organ Recipients
Current Drug Targets Relevance of Excitable Media Theory and Retinal Spreading Depression Experiments in Preclinical Pharmacological Research
Current Neuropharmacology Obstetric Anaesthesia and Obesity
Current Women`s Health Reviews Selective Removal of Macrophages in Atherosclerotic Plaques as a Pharmacological Approach for Plaque Stabilization: Benefits Vs. Potential Complications
Current Vascular Pharmacology Sodium-Glucose Co-Transporter 2 Inhibitors: From Apple Tree to ‘Sweet Pee’
Current Pharmaceutical Design Editorial from Guest Editor: Current Management of Sleep Apnea and Comorbidities
Current Respiratory Medicine Reviews Justification of Increasing the Blood Flow Velocity in the Arteries of the Thyroid Gland in Autoimmune Thyroiditis as a Reflection of Endothelial Changes Due to Inflammatory Status
Current Medical Imaging Transcription Factors in Heart: Promising Therapeutic Targets in Cardiac Hypertrophy
Current Cardiology Reviews Prognostic Utility of Troponin I and N Terminal-ProBNP among Patients with Heart Failure due to Non-Ischemic Cardiomyopathy and Important Correlations
Cardiovascular & Hematological Agents in Medicinal Chemistry A Magnetic Resonance Spectroscopy Study of Lovastatin for Treating Bipolar Mood Disorder: A 4-Week Randomized Double-Blind, Placebo- Controlled Clinical Trial
Recent Patents on Inflammation & Allergy Drug Discovery Organoselenium Compounds as Potential Therapeutic and Chemopreventive Agents: A Review
Current Medicinal Chemistry Vasoprotective Actions of the Atrial Natriuretic Peptide
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Pharmacokinetics of Antifungal Agents in Neonates and Young Infants
Current Medicinal Chemistry Current Evaluation of the Millennium Phytomedicine- Ginseng (II): Collected Chemical Entities, Modern Pharmacology, and Clinical Applications Emanated from Traditional Chinese Medicine
Current Medicinal Chemistry Targeting Cytotoxic Conjugates of Somatostatin, Luteinizing Hormone- Releasing Hormone and Bombesin to Cancers Expressing Their Receptors: A “Smarter” Chemotherapy
Current Pharmaceutical Design