Abstract
Adenosine, a widely distributed modulator, regulates many physiological functions through specific cell membrane G-protein-coupled receptors classified as A1, A2A, A2B and A3. An intense medicinal chemistry effort made over the last 20 years has led to a variety of selective adenosine receptor agonists and antagonists. In particular, the pyrazolo-triazolo-pyrimidine nucleus has been strongly investigated in the last years by our group. All the modifications performed and a tentative of structure-activity-relationship is reported. In fact, the combination of different substitutions at the N7, N8 and N5 positions afford compounds which showed good affinity and selectivity for the different adenosine receptor subtypes. The data herein summarized, permit to speculate on the use of this nucleus as possible template for the adenosine receptor subtypes.
Keywords: pyrazolo-triazolo-pyrimidine, adenosine receptor, adenosine antagonist, adenosine receptor subtype
Current Pharmaceutical Design
Title: Pyrazolo-Triazolo-Pyrimidine Derivatives as Adenosine Receptor Antagonists: A Possible Template for Adenosine Receptor Subtypes?
Volume: 8 Issue: 26
Author(s): Pier Giovanni Baraldi, Barbara Cacciari, Pier Andrea Borea, Katia Varani, Giorgia Pastorin, Tatiana Da Ros, Mojgan Aghazadeh Tabrizi, Francesca Fruttarolo and Giampiero Spalluto
Affiliation:
Keywords: pyrazolo-triazolo-pyrimidine, adenosine receptor, adenosine antagonist, adenosine receptor subtype
Abstract: Adenosine, a widely distributed modulator, regulates many physiological functions through specific cell membrane G-protein-coupled receptors classified as A1, A2A, A2B and A3. An intense medicinal chemistry effort made over the last 20 years has led to a variety of selective adenosine receptor agonists and antagonists. In particular, the pyrazolo-triazolo-pyrimidine nucleus has been strongly investigated in the last years by our group. All the modifications performed and a tentative of structure-activity-relationship is reported. In fact, the combination of different substitutions at the N7, N8 and N5 positions afford compounds which showed good affinity and selectivity for the different adenosine receptor subtypes. The data herein summarized, permit to speculate on the use of this nucleus as possible template for the adenosine receptor subtypes.
Export Options
About this article
Cite this article as:
Baraldi Giovanni Pier, Cacciari Barbara, Borea Andrea Pier, Varani Katia, Pastorin Giorgia, Da Ros Tatiana, Tabrizi Aghazadeh Mojgan, Fruttarolo Francesca and Spalluto Giampiero, Pyrazolo-Triazolo-Pyrimidine Derivatives as Adenosine Receptor Antagonists: A Possible Template for Adenosine Receptor Subtypes?, Current Pharmaceutical Design 2002; 8 (26) . https://dx.doi.org/10.2174/1381612023392838
DOI https://dx.doi.org/10.2174/1381612023392838 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
- Announcements
Related Articles
-
β-Carboline Alkaloids: Biochemical and Pharmacological Functions
Current Medicinal Chemistry Tumor Necrosis Factor: How to Make a Killer Molecule Tumor-Specific?
Current Cancer Drug Targets Is Mania the Hypertension of the Mood? Discussion of A Hypothesis
Current Neuropharmacology Inhibition of Drug Efflux in Mycobacteria with Phenothiazines and Other Putative Efflux Inhibitors
Recent Patents on Anti-Infective Drug Discovery Novel Immunotherapies for Hematological Malignancies
Current Molecular Pharmacology The Medical Complications of Anorexia Nervosa and Their Treatments
Current Women`s Health Reviews Catatonia: A Narrative Review
Central Nervous System Agents in Medicinal Chemistry A<sub>3</sub> Adenosine Receptor: A Plausible Therapeutic Target for Cardio-Protection in Diabetes
Recent Patents on Cardiovascular Drug Discovery Effect of Depression on Self-Management Behaviors and Health Outcomes in Adults with Type 2 Diabetes
Current Diabetes Reviews Mechanisms and Medical Management of Exercise Intolerance in Hypertrophic Cardiomyopathy
Current Pharmaceutical Design Rac-1 as a New Therapeutic Target in Cerebro- and Cardio-Vascular Diseases
Current Drug Targets Is there a Teratogenicity Risk Associated with Cannabis and Synthetic Cannabimimetics’ (‘Spice’) Intake?
CNS & Neurological Disorders - Drug Targets Food-derived Bioactive Peptides - Opportunities for Designing Future Foods
Current Pharmaceutical Design Therapeutic Strategies for Alzheimer's and Parkinson's Diseases by Means of Drug Delivery Systems
Current Medicinal Chemistry Reviewing the Cardiovascular Complications of HIV Infection After the Introduction of Highly Active Antiretroviral Therapy
Current Drug Targets - Cardiovascular & Hematological Disorders The Pentacyclic Triterpenoids in Herbal Medicines and Their Pharmacological Activities in Diabetes and Diabetic Complications
Current Medicinal Chemistry Microcirculation in Sepsis: New Perspectives
Current Vascular Pharmacology Cardiovascular Effects of EGFR (Epidermal Growth Factor Receptor) Monoclonal Antibodies
Cardiovascular & Hematological Agents in Medicinal Chemistry Actions of Adjunctive Nutritional Antioxidants in Periodontitis and Prevalent Systemic Inflammatory Diseases
Endocrine, Metabolic & Immune Disorders - Drug Targets Update on Diagnostic and Treatment of Uncomplicated and Complicated Malaria in Adults and Selected Vulnerable Populations
Infectious Disorders - Drug Targets