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To identify novel adenosine receptor (AR) ligands based on the chalcone scaffold, herein the synthesis, characterization and in vitro and in silico evaluation of 33 chalcones ( 15 - 36 and 37 - 41 ) and structurally related compounds ( 42 - 47 ) are reported. These compounds were characterized by radioligand binding and GTP shift assays to determine the degree and type of binding affinity, respectively, against rat ( r ) A 1 and A 2A ARs. The chalcone derivatives 24 , 29 , 37 and 38 possessed selective A 1 affinity below 10 µM, and thus, are the most active compounds of the present series; compound 38 was the most potent selective A 1 AR antagonist ( K  i ( r ) = 1.6 µM). The structure-affinity relationships (SAR) revealed that the NH 2 -group at position C3 of ring A of the chalcone scaffold played a key role in affinity, and also, the Br-atom at position C3' on benzylidene ring B. Upon in vitro and in silico evaluation, the novel C3 amino-substituted chalcone derivative 38 -that contains an α,ß-unsaturated carbonyl system and easily allows structural modification-may possibly be a synthon in future drug discovery.

C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range