2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists: The 6-Morpholino Derivatives

A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A , A , A , and A adenosine receptor subtypes. Eleven purines showed potent antagonism at A , A , dual A /A , A /A , or A /A adenosine receptors. Additionally, three c...

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Published inMolecules (Basel, Switzerland) Vol. 29; no. 11; p. 2543
Main Authors Areias, Filipe, Correia, Carla, Rocha, Ashly, Teixeira, Sofia, Castro, Marián, Brea, Jose, Hu, Huabin, Carlsson, Jens, Loza, Maria I, Proença, M Fernanda, Carvalho, M Alice
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 28.05.2024
MDPI
Subjects
2-arylpurine derivatives
Adenine - analogs & derivatives
Adenine - chemistry
Adenine - pharmacology
adenine derivatives
Adenosine
adenosine receptor antagonists
Asthma
Chlorine
CHO Cells
Clinical trials
FDA approval
G protein-coupled receptors
Glaucoma
Heart failure
Humans
Ligands
Molecular Structure
Morpholines - chemistry
Morpholines - pharmacology
Proteins
Purinergic P1 Receptor Antagonists - chemistry
Purinergic P1 Receptor Antagonists - pharmacology
Purines - chemical synthesis
Purines - chemistry
Purines - pharmacology
Receptors, Purinergic P1 - metabolism
Structure-Activity Relationship
Temperature
Spain
2-arylpurine derivatives
G protein-coupled receptors
adenine derivatives
structure-activity relationship
adenosine receptor antagonists
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Summary:A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A , A , A , and A adenosine receptor subtypes. Eleven purines showed potent antagonism at A , A , dual A /A , A /A , or A /A adenosine receptors. Additionally, three compounds showed high affinity without selectivity for any specific adenosine receptor. The structure-activity relationships were made for this group of new compounds. The 9-methylpurine derivatives were generally less potent but more selective, and the 9H-purine derivatives were more potent but less selective. These compounds can be an important source of new biochemical tools and/or pharmacological drugs.
Bibliography:ObjectType-Article-1
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These authors contributed equally to this work.
ISSN:1420-3049
1431-5157
1420-3049
DOI:10.3390/molecules29112543