7-Azaindole derivatives as potential partial nicotinic agonists

We have investigated a series of 7-azaindoles as potential partial agonists of the α4β2 nicotinic acetylcholine receptor (nAChR). Three series of 7-azaindole derivatives have been synthesized and evaluated for rat brain neuronal nicotinic receptor affinity and functional activity. Compound (+)-51 exhibited the most potent nAChR binding (Ki = 10 nM). Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus representing a promising lead for the indications of cognition and smoking cessation.

Graphical abstractA series of 7-azaindoles was investigated as potential partial agonists of the α4β2 nicotinic acetylcholine receptor (nAChR).Figure optionsDownload full-size imageDownload as PowerPoint slide