Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: Identification of candidates for clinical development

Letavic, Michael A., Aluisio, Leah, Atack, John R. ORCID: https://orcid.org/0000-0002-3410-791X, Bonaventure, Pascal, Carruthers, Nicholas I., Dugovic, Christine, Everson, Anita, Feinstein, Mark A., Fraser, Ian C., Hoey, Kenway, Jiang, Xiaohui, Keith, John M., Koudriakova, Tatiana, Leung, Perry, Lord, Brian, Lovenberg, Timothy W., Ly, Kiev S., Morton, Kirsten L., Timothy Motley, S., Nepomuceno, Diane, Rizzolio, Michele, Rynberg, Raymond, Sepassi, Kia and Shelton, Jonathan 2010. Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: Identification of candidates for clinical development. Bioorganic and Medicinal Chemistry Letters 20 (14) , pp. 4210-4214. 10.1016/j.bmcl.2010.05.041

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Abstract

The pre-clinical characterization of novel aryloxypyridine amides that are histamine H3 receptor antagonists is described. These compounds are high affinity histamine H3 ligands that penetrate the CNS and occupy the histamine H3 receptor in rat brain. Several compounds were extensively profiled pre-clinically leading to the identification of two compounds suitable for nomination as development candidates.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Biosciences
Publisher:	Elsevier
ISSN:	0960-894X
Date of Acceptance:	12 May 2010
Last Modified:	03 Nov 2022 09:45
URI:	https://orca.cardiff.ac.uk/id/eprint/105897

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