Cargando…

Piperazine- and Piperidine-Containing Thiazolo[5,4-d]pyrimidine Derivatives as New Potent and Selective Adenosine A(2A) Receptor Inverse Agonists

The therapeutic use of A(2A) adenosine receptor (AR) antagonists for the treatment of neurodegenerative disorders, such as Parkinson and Alzheimer diseases, is a very promising approach. Moreover, the potential therapeutic role of A(2A) AR antagonists to avoid both immunoescaping of tumor cells and...

Descripción completa

Detalles Bibliográficos
Autores principales:	Varano, Flavia, Catarzi, Daniela, Vigiani, Erica, Vincenzi, Fabrizio, Pasquini, Silvia, Varani, Katia, Colotta, Vittoria
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	MDPI 2020
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7465344/ https://www.ncbi.nlm.nih.gov/pubmed/32722122 http://dx.doi.org/10.3390/ph13080161

Ejemplares similares

Design and Synthesis of Novel Thiazolo[5,4-d]pyrimidine Derivatives with High Affinity for Both the Adenosine A(1) and A(2A) Receptors, and Efficacy in Animal Models of Depression
por: Varano, Flavia, et al.
Publicado: (2021)

Amino-3,5-Dicyanopyridines Targeting the Adenosine Receptors. Ranging from Pan Ligands to Combined A1/A2B Partial Agonists
por: Catarzi, Daniela, et al.
Publicado: (2019)

4-Heteroaryl Substituted Amino-3,5-Dicyanopyridines as New Adenosine Receptor Ligands: Novel Insights on Structure-Activity Relationships and Perspectives
por: Catarzi, Daniela, et al.
Publicado: (2022)

The role of 5-arylalkylamino- and 5-piperazino- moieties on the 7-aminopyrazolo[4,3-d]pyrimidine core in affecting adenosine A(1) and A(2A) receptor affinity and selectivity profiles
por: Squarcialupi, Lucia, et al.
Publicado: (2017)

Special Issue “Adenosine Receptors as Attractive Targets in Human Diseases”
por: Catarzi, Daniela, et al.
Publicado: (2021)

Inhibition of A(2A) Adenosine Receptor Signaling in Cancer Cells Proliferation by the Novel Antagonist TP455
por: Gessi, Stefania, et al.
Publicado: (2017)

Adenosine and Inflammation: Here, There and Everywhere
por: Pasquini, Silvia, et al.
Publicado: (2021)

Targeting Adenosine Receptors: A Potential Pharmacological Avenue for Acute and Chronic Pain
por: Vincenzi, Fabrizio, et al.
Publicado: (2020)

Identification of Novel Thiazolo[5,4-b]Pyridine Derivatives as Potent Phosphoinositide 3-Kinase Inhibitors
por: Xia, Liang, et al.
Publicado: (2020)

Pharmacological Characterization of P626, a Novel Dual Adenosine A(2A)/A(2B) Receptor Antagonist, on Synaptic Plasticity and during an Ischemic-like Insult in CA1 Rat Hippocampus
por: Venturini, Martina, et al.
Publicado: (2023)

Update on the recent development of allosteric modulators for adenosine receptors and their therapeutic applications
por: Pasquini, Silvia, et al.
Publicado: (2022)

Adenosine Receptors in Neuropsychiatric Disorders: Fine Regulators of Neurotransmission and Potential Therapeutic Targets
por: Pasquini, Silvia, et al.
Publicado: (2022)

A(1) Adenosine Receptor Partial Agonists and Allosteric Modulators: Advancing Toward the Clinic?
por: Vincenzi, Fabrizio, et al.
Publicado: (2020)

Anxiolytic properties of A(1) adenosine receptor PAMs
por: Vincenzi, Fabrizio, et al.
Publicado: (2016)

Pharmacology of Adenosine Receptors: Recent Advancements
por: Vincenzi, Fabrizio, et al.
Publicado: (2023)

A(3) Adenosine and P2X7 Purinergic Receptors as New Targets for an Innovative Pharmacological Therapy of Malignant Pleural Mesothelioma
por: Vincenzi, Fabrizio, et al.
Publicado: (2021)

An Open Question: Is the A(2A) Adenosine Receptor a Novel Target for Alzheimer’s Disease Treatment?
por: Merighi, Stefania, et al.
Publicado: (2021)

A(2A) Adenosine Receptor as a Potential Biomarker and a Possible Therapeutic Target in Alzheimer’s Disease
por: Gessi, Stefania, et al.
Publicado: (2021)

A(2A) Adenosine Receptor: A Possible Therapeutic Target for Alzheimer’s Disease by Regulating NLRP3 Inflammasome Activity?
por: Merighi, Stefania, et al.
Publicado: (2022)

The Detrimental Action of Adenosine on Glutamate-Induced Cytotoxicity in PC12 Cells Can Be Shifted towards a Neuroprotective Role through A(1)AR Positive Allosteric Modulation
por: Vincenzi, Fabrizio, et al.
Publicado: (2020)

A(2A )and A(3 )adenosine receptor expression in rheumatoid arthritis: upregulation, inverse correlation with disease activity score and suppression of inflammatory cytokine and metalloproteinase release
por: Varani, Katia, et al.
Publicado: (2011)

“Dual Anta-Inhibitors” of the A(2A) Adenosine Receptor and Casein Kinase CK1delta: Synthesis, Biological Evaluation, and Molecular Modeling Studies
por: Spinaci, Andrea, et al.
Publicado: (2023)

Caffeine for Prevention of Alzheimer’s Disease: Is the A(2A) Adenosine Receptor Its Target?
por: Merighi, Stefania, et al.
Publicado: (2023)

Strategies for Drug Delivery into the Brain: A Review on Adenosine Receptors Modulation for Central Nervous System Diseases Therapy
por: Fernandez, Mercedes, et al.
Publicado: (2023)

Synthesis of New Thiazolo[4,5-d]pyrimidines as Corticotropin Releasing Factor Modulators
por: Kuppast, Bhimanna, et al.
Publicado: (2015)

Synthesis of Pyrimidine Incorporated Piperazine Derivatives and their Antimicrobial Activity
por: Thriveni, K. S., et al.
Publicado: (2014)

Crystal structures of 4-(pyrimidin-2-yl)piperazin-1-ium chloride and 4-(pyrimidin-2-yl)piperazin-1-ium nitrate
por: Yamuna, Thammarse S., et al.
Publicado: (2014)

Adenosine Receptors as a Biological Pathway for the Anti-Inflammatory and Beneficial Effects of Low Frequency Low Energy Pulsed Electromagnetic Fields
por: Varani, Katia, et al.
Publicado: (2017)

Role and Function of A(2A) and A(3) Adenosine Receptors in Patients with Ankylosing Spondylitis, Psoriatic Arthritis and Rheumatoid Arthritis
por: Ravani, Annalisa, et al.
Publicado: (2017)

Design and Synthesis of Thiazolo[5,4-f]quinazolines as DYRK1A Inhibitors, Part I
por: Foucourt, Alicia, et al.
Publicado: (2014)

Design and Synthesis of Thiazolo[5,4-f]quinazolines as DYRK1A Inhibitors, Part II
por: Foucourt, Alicia, et al.
Publicado: (2014)

Identification of Thiazolo[5,4-b]pyridine Derivatives as c-KIT Inhibitors for Overcoming Imatinib Resistance
por: Nam, Yunju, et al.
Publicado: (2022)

Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity
por: De Luca, Laura, et al.
Publicado: (2023)

Investigation of Structure–Activity Relationships for Benzoyl and Cinnamoyl Piperazine/Piperidine Amides as Tyrosinase Inhibitors
por: Varela, Marina T., et al.
Publicado: (2023)

Design and synthesis of some substituted thiazolo[3,2-a]pyrimidine derivatives of potential biological activities
por: Abdel Moty, Samia G., et al.
Publicado: (2016)

Hexafluoroisopropanol-Mediated Domino Reaction for the Synthesis of Thiazolo-androstenones: Potent Anticancer Agents
por: Okolo, ChrisTina, et al.
Publicado: (2018)

4-Methyl-6-(piperidin-1-yl)pyrimidin-2-amine
por: Sreenivasa, S., et al.
Publicado: (2013)

Synthesis, Crystal Structure, and Biological Evaluation of Fused Thiazolo[3,2-a]Pyrimidines as New Acetylcholinesterase Inhibitors
por: Mahgoub, Mohamed Y., et al.
Publicado: (2019)

Regioselective convergent synthesis of 2-arylidene thiazolo[3,2-a]pyrimidines as potential anti-chikungunya agents
por: Fares, Mohamed, et al.
Publicado: (2020)

Design, synthesis, docking, and anticancer evaluations of new thiazolo[3,2-a] pyrimidines as topoisomerase II inhibitors
por: El-Zoghbi, Mona S., et al.
Publicado: (2023)

Cannot write session to /tmp/vufind_sessions/sess_2p4pb7c0hktlqap1qujlqf84qd