Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376906 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
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
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,