Cited 3 times since 2007 (0.2 per year) source: EuropePMC Bioorganic & medicinal chemistry letters, Volume 18, Issue 1, 1 1 2007, Pages 188-193 7-Azaindole derivatives as potential partial nicotinic agonists. Stoit AR, den Hartog AP, Mons H, van Schaik S, Barkhuijsen N, Stroomer C, Coolen HK, Reinders JH, Adolfs TJ, van der Neut M, Keizer H, Kruse CG
We have investigated a series of 7-azaindoles as potential partial agonists of the alpha4beta2 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.
