2-Phenylimidazo [2, 1-i] purin-5-ones: structure–activity relationships and characterization of potent and selective inverse agonists at human A3 adenosine receptors

V Ozola, M Thorand, M Diekmann, R Qurishi…

Index: Ozola, Vita; Thorand, Mark; Diekmann, Martina; Qurishi, Ramatullah; Schumacher, Britta; Jacobson, Kenneth A.; Mueller, Christa E. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 3 p. 347 - 356

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Citation Number: 41

Abstract

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 ...