1204606-82-5Relevant articles and documents
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: Identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-Fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1- ylbutyl) Urea (SEN34625/WYE-103914)
Ghiron, Chiara,Haydar, Simon N.,Aschmies, Suzan,Bothmann, Hendrick,Castaldo, Cristiana,Cocconcelli, Giuseppe,Comery, Thomas A.,Di, Li,Dunlop, John,Lock, Tim,Kramer, Angela,Kowal, Dianne,Jow, Flora,Grauer, Steve,Harrison, Boyd,La Rosa, Salvatore,MacCari, Laura,Marquis, Karen L.,Micco, Iolanda,Nencini, Arianna,Quinn, Joanna,Robichaud, Albert J.,Roncarati, Renza,Scali, Carla,Terstappen, Georg C.,Turlizzi, Elisa,Valacchi, Michela,Varrone, Maurizio,Zanaletti, Riccardo,Zanelli, Ugo
supporting information; experimental part, p. 4379 - 4389 (2010/09/04)
Alpha-7 nicotinic acetylcholine receptor (α7 nAChR) agonists are promising therapeutic candidates for the treatment of cognitive impairment. We report a series of novel, potent small molecule agonists (4-18) of the α7 nAChR deriving from our continuing efforts in the areas of Alzheimer's disease and schizophrenia. One of the compounds of the series containing a urea moiety (16) was further shown to be a selective agonist of the α7 nAChR with excellent in vitro and in vivo profiles, brain penetration, and oral bioavailability and demonstrated in vivo efficacy in multiple behavioral cognition models. Structural modifications leading to the improved selectivity profile and the biological evaluation of this series of compounds are discussed.
ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR INHIBITORS
-
Page/Page column 23, (2010/02/17)
The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
