Benzopyrone represents a privilege scaffold to identify novel adenosine A1/A2A receptor antagonists.

摘要: Abstract Adenosine receptor antagonists are under investigation as potential drug candidates for the treatment of certain cancers, neurological disorders, depression and potentially improve tumour immunotherapy. The benzo-γ-pyrone scaffold is well-known in medicinal chemistry with diverse pharmacological activities attributed to them, however, their therapeutic adenosine have not been investigated detail. To expand on structure–activity relationships, present study explored A1 A2A binding affinities a selected series analogues. In vitro evaluation led identification 5-hydroxy-2-(3-hydroxyphenyl)-4H-1-benzopyran-4-one best affinity among test compounds was found be non-selective (A1Ki = 0.956 µM; A2AKi = 1.44 µM). Hydroxy substitution ring A and/or B play key role modulating at receptors. increased nanomolar range hydroxy C6 (ring A), while meta-hydroxy governed affinity. double bond between C2 C3 C well phenyl shown imperative both Selected derivatives behaved performed GTP shift assays. It may concluded that based suitable leads designing identifying various disorders.