Medicinal Chemistry of A3 Adenosine Receptor Modulators: Pharmacological Activities and Therapeutic Implications

PG Baraldi, D Preti, PA Borea… - Journal of medicinal …, 2012 - ACS Publications
The purine nucleoside adenosine is identified as a ubiquitous molecule regulator of different
tissues and cell functions. 1 Adenosine is generated in the extracellular space by the …

Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure− Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy …

M Stampelou, A Suchankova, E Tzortzini… - Journal of Medicinal …, 2022 - ACS Publications
Drugs targeting adenosine receptors (AR) can provide treatment for diseases. We report the
identification of 7-(phenylamino)-pyrazolo [3, 4-c] pyridines L2–L10, A15, and A17 as low …

Pyrazolo [4, 3-e][1, 2, 4] triazolo [1, 5-c] pyrimidines and structurally simplified analogs. Chemistry and SAR profile as adenosine receptor antagonists

S Redenti, A Ciancetta, G Pastorin… - Current Topics in …, 2016 - ingentaconnect.com
Adenosine was defined as a neuromodulator which exerts its action by interaction with
specific G-protein coupled receptor termed adenosine receptors. Adenosine receptors are …

Simplified molecular input line entry system-based optimal descriptors: QSAR modelling for voltage-gated potassium channel subunit Kv7. 2

PGR Achary - SAR and QSAR in Environmental Research, 2014 - Taylor & Francis
CORAL software has been used to build quantitative structure–activity relationships
(QSARs) for the prediction of binding affinities (pEC50, ie, minus decimal logarithm of the …

Medicinal Chemistry of A2B Adenosine Receptors

CE Müller, Y Baqi, S Hinz, V Namasivayam - The adenosine receptors, 2018 - Springer
Abstract A 2B adenosine receptors (A 2B ARs) are in the focus of interest as drug targets in
(immuno) oncology since antagonists show anti-proliferative, anti-angiogenic, anti …

Discovery of a High Affinity Adenosine A1/A3 Receptor Antagonist with a Novel 7-Amino-pyrazolo[3,4-d]pyridazine Scaffold

A Suchankova, M Stampelou, K Koutsouki… - ACS Medicinal …, 2022 - ACS Publications
Here we describe the design and synthesis of pyrazolo [3, 4-d] pyridazines as adenosine
receptor (AR) ligands. We demonstrate that the introduction of a 3-phenyl group, together …

Exploration of chalcones and related heterocycle compounds as ligands of adenosine receptors: therapeutics development

C Matthee, G Terre'Blanche, LJ Legoabe… - Molecular Diversity, 2022 - Springer
Adenosine receptors (ARs) are ubiquitously distributed throughout the mammalian body
where they are involved in an extensive list of physiological and pathological processes that …

8-(2-Furyl) adenine derivatives as A2A adenosine receptor ligands

D Dal Ben, M Buccioni, C Lambertucci… - European Journal of …, 2013 - Elsevier
Selective adenosine receptor modulators are potential tools for numerous therapeutic
applications, including cardiovascular, inflammatory, and neurodegenerative diseases. In …

Insight into the binding mode and the structural features of the pyrimidine derivatives as human A2A adenosine receptor antagonists

L Zhang, T Liu, X Wang, J Wang, G Li, Y Li, L Yang… - Biosystems, 2014 - Elsevier
The interaction of 278 monocyclic and bicyclic pyrimidine derivatives with human A 2A
adenosine receptor (AR) was investigated by employing molecular dynamics …

[HTML][HTML] Synthesis of 1H-pyrazolo [3, 4-d] pyrimidines via solid-phase Aza-Wittig/electrocyclic ring closure reaction

S Liao, L Xing, B Hamper - Tetrahedron Letters, 2013 - Elsevier
An elegant solid-phase synthetic route of pyrazolo [3, 4-d] pyrimidine derivatives via Aza-
Wittig/electrocyclic ring closure reaction was developed and validated. By manipulating the …