| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373068 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
A new family of Histamine H3 receptor antagonists (5a–t) has been prepared based on the structure of the natural product Conessine, a known H3 antagonist. Several members of the new series are highly potent and selective binders of rat and human H3 receptors and display inverse agonism at the human H3 receptor. Compound 5n exhibited promising rat pharmacokinetic properties and demonstrated functional antagonism of the H3 receptor in an in-vivo pharmacological model.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Vincent J. Santora, Jonathan A. Covel, Rena Hayashi, Brian J. Hofilena, Jason B. Ibarra, Michelle D. Pulley, Michael I. Weinhouse, Dipanjan Sengupta, Jonathan J. Duffield, Graeme Semple, Robert R. Webb, Carleton Sage, Albert Ren, Guilherme Pereira,