e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
2-Phenylimidazo [2, 1-i] purin-5-ones: structure–activity relationships and characterization of potent and selective inverse agonists at human A3 adenosine receptors
Structure–activity relationships of 2-phenyl-imidazo [2, 1-i] purin-5-ones as ligands for human A3 adenosine receptors (ARs) were investigated. An ethyl group in the 8-position of the imidazoline ring of 4-methyl-2-phenyl-imidazopurinone leading to chiral compounds was found to increase affinity for human A3 ARs by several thousand-fold. Propyl substitution instead of methyl at N4 decreased A3 affinity but increased A1 affinity leading to potent A1 ...
