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 in | Molecules (Basel, Switzerland) Vol. 29; no. 11; p. 2543 |
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Main Authors | , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Switzerland
MDPI AG
28.05.2024
MDPI |
Subjects | |
Online Access | Get full text |
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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. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 These authors contributed equally to this work. |
ISSN: | 1420-3049 1431-5157 1420-3049 |
DOI: | 10.3390/molecules29112543 |