Journal article
4,5-Dihydropyridazin-3-one derivatives as histamine H-3 receptor inverse agonists
Bioorganic & medicinal chemistry letters, v 22(1), pp 194-198
01 Jan 2012
PMID: 22142542
Featured in Collection : UN Sustainable Development Goals @ Drexel
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. (C) 2011 Elsevier Ltd. All rights reserved.
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Details
- Title
- 4,5-Dihydropyridazin-3-one derivatives as histamine H-3 receptor inverse agonists
- Creators
- Robert L. Hudkins - Cephalon Inc, Discovery Res, W Chester, PA 19380 USALisa D. Aimone - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAReddeppa Reddy Dandu - Cephalon Inc, Discovery Res, W Chester, PA 19380 USADerek Dunn - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAJohn A. Gruner - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAZeqi Huang - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAKurt A. Josef - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAJacquelyn A. Lyons - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAJoanne R. Mathiasen - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAMing Tao - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAAllison L. Zulli - Cephalon Inc, Discovery Res, W Chester, PA 19380 USARita Raddatz - Cephalon Inc, Discovery Res, W Chester, PA 19380 USA
- Publication Details
- Bioorganic & medicinal chemistry letters, v 22(1), pp 194-198
- Publisher
- Elsevier
- Number of pages
- 5
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000298636700033
- Scopus ID
- 2-s2.0-84655174952
- Other Identifier
- 991021900194004721
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InCites Highlights
Data related to this publication, from InCites Benchmarking & Analytics tool:
- Web of Science research areas
- Chemistry, Medicinal
- Chemistry, Organic