2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists: The 6-Morpholino Derivatives
oleh: Filipe Areias, Carla Correia, Ashly Rocha, Sofia Teixeira, Marián Castro, Jose Brea, Huabin Hu, Jens Carlsson, Maria I. Loza, M. Fernanda Proença, M. Alice Carvalho
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2024-05-01 |
Deskripsi
A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A<sub>1</sub>, A<sub>2A</sub>, A<sub>2B</sub>, and A<sub>3</sub> adenosine receptor subtypes. Eleven purines showed potent antagonism at A<sub>1</sub>, A<sub>3</sub>, dual A<sub>1</sub>/A<sub>2A</sub>, A<sub>1</sub>/A<sub>2B</sub>, or A<sub>1</sub>/A<sub>3</sub> 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.