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Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists

Stocking, Emily M., Aluisio, Leah, Atack, John R., Bonaventure, Pascal, Carruthers, Nicholas I., Dugovic, Christine, Everson, Anita, Fraser, Ian, Jiang, Xiaohui, Leung, Perry, Lord, Brian, Ly, Kiev S., Morton, Kirsten L., Nepomuceno, Diane, Shah, Chandravadan R., Shelton, Jonathan, Soyode-Johnson, Akinola and Letavic, Michael A. 2010. Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists. Bioorganic and Medicinal Chemistry Letters 20 (9) , pp. 2755-2760. 10.1016/j.bmcl.2010.03.071

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Abstract

Pre-clinical characterization of novel substituted pyrrolidines that are high affinity histamine H3 receptor antagonists is described. These compounds efficiently penetrate the CNS and occupy the histamine H3 receptor in rat brain following oral administration. One compound, (2S,4R)-1-[2-(4-cyclobutyl-[1,4]diazepane-1-carbonyl)-4-(3-fluoro-phenoxy)-pyrrolidin-1-yl]-ethanone, was extensively profiled and shows promise as a potential clinical candidate.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Publisher: Elsevier
ISSN: 0960-894X
Date of Acceptance: 17 March 2010
Last Modified: 14 Nov 2017 21:02
URI: http://orca.cf.ac.uk/id/eprint/105898

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