Effect of Nitrogen Atom Substitution in A3 Adenosine Receptor Binding: N-(4,6-Diarylpyridin-2-yl)acetamides as Potent and Selective Antagonists

2017 ◽  
Vol 60 (17) ◽  
pp. 7502-7511 ◽  
Author(s):  
Jhonny Azuaje ◽  
Willem Jespers ◽  
Vicente Yaziji ◽  
Ana Mallo ◽  
María Majellaro ◽  
...  
Keyword(s):  
Nitrogen Atom ◽  
Receptor Binding ◽  
Adenosine Receptor ◽  
Selective Antagonists ◽  
A3 Adenosine Receptor

ChemInform Abstract: Introduction of Alkynyl Chains on C-8 of Adenosine Led to Very Selective Antagonists of the A3 Adenosine Receptor.

ChemInform ◽  
2010 ◽  
Vol 32 (46) ◽  
pp. no-no ◽  
Author(s):  
Rosaria Volpini ◽  
Stefano Costanzi ◽  
Catia Lambertucci ◽  
Sauro Vittori ◽  
K.-N. Klotz ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Selective Antagonists ◽  
A3 Adenosine Receptor

Conversion of A3 Adenosine Receptor Agonists into Selective Antagonists by Modification of the 5′-Ribofuran-uronamide Moiety.

ChemInform ◽  
2006 ◽  
Vol 37 (18) ◽  
Author(s):  
Zhan-Guo Gao ◽  
Bhalchandra V. Joshi ◽  
Athena M. Klutz ◽  
Soo-Kyung Kim ◽  
Hyuk Woo Lee ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Adenosine Receptor Agonists ◽  
Receptor Agonists ◽  
Selective Antagonists ◽  
A3 Adenosine Receptor

scholarly journals Design and Synthesis of 2,6-Disubstituted-4′-Selenoadenosine-5′-N,N-Dimethyluronamide Derivatives as Human A3 Adenosine Receptor Antagonists

2021 ◽  
Vol 14 (4) ◽  
pp. 363
Author(s):  
Hongseok Choi ◽  
Kenneth A. Jacobson ◽  
Jinha Yu ◽  
Lak Shin Jeong
Keyword(s):  
Binding Affinity ◽  
Adenosine Receptor ◽  
Functional Assay ◽  
Antagonist Activity ◽  
Methyl Group ◽  
Design And Synthesis ◽  
Selective Antagonists ◽  
A3 Adenosine Receptor ◽  
High Binding Affinity

A new series of 4′-selenoadenosine-5′-N,N-dimethyluronamide derivatives as highly potent and selective human A3 adenosine receptor (hA3AR) antagonists, is described. The highly selective A3AR agonists, 4′-selenoadenosine-5′-N-methyluronamides were successfully converted into selective antagonists by adding a second N-methyl group to the 5′-uronamide position. All the synthesized compounds showed medium to high binding affinity at the hA3AR. Among the synthesized compounds, 2-H-N6-3-iodobenzylamine derivative 9f exhibited the highest binding affinity at hA3AR. (Ki = 22.7 nM). The 2-H analogues generally showed better binding affinity than the 2-Cl analogues. The cAMP functional assay with 2-Cl-N6-3-iodobenzylamine derivative 9l demonstrated hA3AR antagonist activity. A molecular modelling study suggests an important role of the hydrogen of 5′-uronamide as an essential hydrogen bonding donor for hA3AR activation.

scholarly journals Exploring distal regions of the A3 adenosine receptor binding site: sterically constrained N6-(2-phenylethyl)adenosine derivatives as potent ligands

2004 ◽  
Vol 12 (9) ◽  
pp. 2021-2034 ◽  
Author(s):  
Susanna Tchilibon ◽  
Soo-Kyung Kim ◽  
Zhan-Guo Gao ◽  
Brian A Harris ◽  
Joshua B Blaustein ◽  
...  
Keyword(s):  
Binding Site ◽  
Receptor Binding ◽  
Adenosine Receptor ◽  
Receptor Binding Site ◽  
A3 Adenosine Receptor ◽  
Adenosine Derivatives

scholarly journals Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A3 adenosine receptor antagonists

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1920-1932 ◽  
Author(s):  
Jinha Yu ◽  
Philip Mannes ◽  
Young-Hwan Jung ◽  
Antonella Ciancetta ◽  
Amelia Bitant ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Receptor Antagonists ◽  
Agonist Affinity ◽  
Structure Activity ◽  
Selective Antagonists ◽  
A3 Adenosine Receptor ◽  
Relationship Of ◽  
Adenine Derivatives

Adenines that incorporate known agonist affinity-enhancing substituents are A3AR-selective antagonists.

scholarly journals Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5′-ribofuran-uronamide moiety

2006 ◽  
Vol 16 (3) ◽  
pp. 596-601 ◽  
Author(s):  
Zhan-Guo Gao ◽  
Bhalchandra V. Joshi ◽  
Athena M. Klutz ◽  
Soo-Kyung Kim ◽  
Hyuk Woo Lee ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Adenosine Receptor Agonists ◽  
Receptor Agonists ◽  
Selective Antagonists ◽  
A3 Adenosine Receptor

scholarly journals Novel fluorescent antagonist as a molecular probe in A3 adenosine receptor binding assays using flow cytometry

2012 ◽  
Vol 83 (11) ◽  
pp. 1552-1561 ◽  
Author(s):  
Eszter Kozma ◽  
T. Santhosh Kumar ◽  
Stephanie Federico ◽  
Khai Phan ◽  
Ramachandran Balasubramanian ◽  
...  
Keyword(s):  
Flow Cytometry ◽  
Receptor Binding ◽  
Adenosine Receptor ◽  
Molecular Probe ◽  
Binding Assays ◽  
A3 Adenosine Receptor

scholarly journals Pharmacological characterization of novel A3 adenosine receptor-selective antagonists

1997 ◽  
Vol 36 (9) ◽  
pp. 1157-1165 ◽  
Author(s):  
Kenneth A. Jacobson ◽  
Kyung-Sun Park ◽  
Ji-Long Jiang ◽  
Yong-Chul Kim ◽  
Mark E. Olah ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Pharmacological Characterization ◽  
Selective Antagonists ◽  
A3 Adenosine Receptor
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