Imidazo[1,2-α]pyridines possess adenosine A1 receptor affinity for the potential treatment of cognition in neurological disorders

摘要: Abstract Previous research has shown that bicyclic 6:5-fused heteroaromatic compounds with two N -atoms have variable degrees of adenosine A 1 receptor antagonistic activity. Prompted by this imidazo[1,2-α]pyridine analogues were synthesized and evaluated for their 2A affinity via radioligand binding studies subjected to a GTP shift assay determine its agonistic or functionality. Imidazo[1,2-α]pyridine, the parent scaffold, was found devoid receptors. The influence substitution on position C2 showed no improvement either affinity. addition an amino cyclohexylamino group C3 also Surprisingly para -substitution phenyl ring at in combination led low micromolar range compound 4d showing: (1) highest K i value 2.06 µM (2) properties. This pilot study concludes -substituted 3-cyclohexylamino-2-phenyl-imidazo[1,2-α]pyridine represent interesting scaffold investigate further structure-activity relationships design novel imidazo[1,2-α]pyridine-based antagonists treatment neurodegenerative disorders.