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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/DReceptor antagonist

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 and Zonzini, Laura 2010. 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/DReceptor antagonist. Journal of Medicinal Chemistry 53 (23) , pp. 8228-8240. 10.1021/jm100714c

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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-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (36) was found to combine potent in vivo activity with a strong preclinical developability profile, and on this basis it was selected as a drug candidate with the aim of assessing its potential as a fast-onset antidepressant/anxiolytic.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Medicine
Publisher: ACS Publications
ISSN: 0022-2623
Last Modified: 21 Feb 2018 10:51
URI: http://orca-mwe.cf.ac.uk/id/eprint/109337

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