Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593126 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
H3R structure-activity relationships for a new class of 4,5-dihydropyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modification of the 4,5-dihydropyridazinone moiety to block in vivo metabolism identified 4,4-dimethyl-6-{4-[3-((R)-2-methyl-pyrrolidin-1-yl)-propoxy]-phenyl}-4,5-dihydro-2H-pyridazin-3-one 22 as a lead candidate demonstrating potent in vivo functional H3R antagonism in the rat dipsogenia model and robust wake promoting activity in the rat EEG/EMG model.
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Authors
Robert L. Hudkins, Lisa D. Aimone, Reddeppa reddy Dandu, Derek Dunn, John A. Gruner, Zeqi Huang, Kurt A. Josef, Jacquelyn A. Lyons, Joanne R. Mathiasen, Ming Tao, Allison L. Zulli, Rita Raddatz,