| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371772 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
Structure-activity relationship on a novel ketone class of H3R antagonists/inverse agonists is disclosed. Compound 4 showed excellent target potency, selectivity and brain penetration. Evaluation of antagonist 4 in the rat EEG/EMG model demonstrated robust wake activity thereby establishing preclinical proof of concept.
Related Topics
Physical Sciences and Engineering
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Organic Chemistry
Authors
Babu G. Sundar, Thomas R. Bailey, Derek Dunn, Greg A. Hostetler, Sankar Chatterjee, Edward R. Bacon, Christoph Yue, Dominique Schweizer, Lisa D. Aimone, John A. Gruner, Jacquelyn Lyons, Rita Raddatz, Brigitte Lesur,