- 7-Azaindole derivatives as potential partial nicotinic agonists.
7-Azaindole derivatives as potential partial nicotinic agonists.
Bioorganic & medicinal chemistry letters (2007-11-17)
Axel R Stoit, Arnold P den Hartog, Harry Mons, Sjoerd van Schaik, Nynke Barkhuijsen, Cees Stroomer, Hein K A C Coolen, Jan Hendrik Reinders, Tiny J P Adolfs, Martina van der Neut, Hiskias Keizer, Chris G Kruse
PMID18006307
ABSTRACT
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.