New insight into adenosine receptors selectivity derived from a novel series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamides and furamides
Copyright policy )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. Compounds 5a and 5g showed moderate selectivity for A2A adenosine receptors. Molecular docking versus all four human adenosine receptors combined with membrane molecular dynamics studies were performed to rationalise the peculiar selectivity profile of 5d antagonist.
Models, Molecular, Binding Sites, Molecular Structure, Purinergic Antagonists, Receptor, Adenosine A2A, Molecular Conformation, Receptors, Purinergic P1, CHO Cells, Amides, Binding, Competitive, Adenosine A2 Receptor Antagonists, Protein Structure, Tertiary, Radioligand Assay, Cricetulus, Models, Chemical, Cricetinae, Benzamides, Animals, Humans, Furans
Models, Molecular, Binding Sites, Molecular Structure, Purinergic Antagonists, Receptor, Adenosine A2A, Molecular Conformation, Receptors, Purinergic P1, CHO Cells, Amides, Binding, Competitive, Adenosine A2 Receptor Antagonists, Protein Structure, Tertiary, Radioligand Assay, Cricetulus, Models, Chemical, Cricetinae, Benzamides, Animals, Humans, Furans
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