7-Azaindole derivatives as potential partial nicotinic agonists

AR Stoit, AP den Hartog, H Mons, S van Schaik…

Index: Stoit, Axel R.; den Hartog, Arnold P.; Mons, Harry; van Schaik, Sjoerd; Barkhuijsen, Nynke; Stroomer, Cees; Coolen, Hein K.A.C.; Reinders, Jan Hendrik; Adolfs, Tiny J.P.; van der Neut, Martina; Keizer, Hiskias; Kruse, Chris G. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 188 - 193

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Citation Number: 12

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= 10nM). Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus ...