Stocking, Emily M., Aluisio, Leah, Atack, John R. ORCID: https://orcid.org/0000-0002-3410-791X, 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 |
Official URL: http://dx.doi.org/10.1016/j.bmcl.2010.03.071
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 |
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Date Type: | Publication |
Status: | Published |
Schools: | Biosciences |
Publisher: | Elsevier |
ISSN: | 0960-894X |
Date of Acceptance: | 17 March 2010 |
Last Modified: | 03 Nov 2022 09:45 |
URI: | https://orca.cardiff.ac.uk/id/eprint/105898 |
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