New insight into adenosine receptors selectivity derived from a novel series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamides and furamides.

A series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamide and furamide analogues were investigated in radioligand binding studies at adenosine receptor subtypes with an aim to obtain potent and selective adenosine receptor ligands. Benzamide and furamide linked to thiazole was found to be crucial for high adenosine receptor affinity. The most potent compound indentified in this study was 5d with low nanomolar affinity for all four adenosine receptor subtypes.

Pair wise binding affinity: 3D QSAR studies on a set of triazolo [1, 5-a] quinoxalines as antagonists of AMPA and KA receptors.

The glutamate receptor system is implicated in the development and maintenance of epileptic seizures and it has been reported that compounds showing high affinity for both AMPA and KA binding sites are more potent anticonvulsants than compounds having selective affinity toward AMPA or KA receptor. These outcomes make such inhibitors future potential antiepileptic drugs. So, the pair wise binding affinity for AMPA and KA receptors inhibition was proposed by using the addition between biological activities of ligands.