| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374257 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
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.
Graphical abstractSubstituted pyrrolidines are potent histamine H3 antagonists with favorable drug-like properties.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Emily M. Stocking, Leah Aluisio, John R. Atack, Pascal Bonaventure, Nicholas I. Carruthers, Christine Dugovic, Anita Everson, Ian Fraser, Xiaohui Jiang, Perry Leung, Brian Lord, Kiev S. Ly, Kirsten L. Morton, Diane Nepomuceno, Chandravadan R. Shah,