Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl] ethyl} phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT1A/B/D …

…, MJ Garnier, A Jaxa-Chamiec, G Manchee…

Index: Leslie, Colin P.; Biagetti, Matteo; Bison, Silvia; Bromidge, Steven M.; Di Fabio, Romano; Donati, Daniele; Falchi, Alessandro; Garnier, Martine J.; Jaxa-Chamiec, Albert; Manchee, Gary; Merlo, Giancarlo; Pizzi, Domenica A.; Stasi, Luigi P.; Tibasco, Jessica; Vong, Antonio; Ward, Simon E.; Zonzini, Laura Journal of Medicinal Chemistry, 2010 , vol. 53, # 23 p. 8228 - 8240

Full Text: HTML

Citation Number: 7

Abstract

In an effort to identify selective drug like pan-antagonists of the 5-HT1 autoreceptors, studies were conducted to elaborate a previously reported dual acting 5-HT1 antagonist/SSRI structure. A novel series of compounds was identified showing low intrinsic activities and potent affinities across the 5-HT1A, 5-HT1B, and 5-HT1D receptors as well as high selectivity against the serotonin transporter. From among these compounds, 1-(3-{2-[4-(2- ...