Journal article
Identification of pyridazin-3-one derivatives as potent, selective histamine H-3 receptor inverse agonists with robust wake activity
Bioorganic & medicinal chemistry letters, v 21(18), pp 5493-5497
15 Sep 2011
PMID: 21782432
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
H3R structure-activity relationships on a novel class of pyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules with excellent target potency, selectivity and pharmacokinetic properties. Compounds 13 and 21 displayed potent functional H3R antagonism in vivo in the rat dipsogenia model and demonstrated robust wake activity in the rat EEG/EMG model. (C) 2011 Elsevier Ltd. All rights reserved.
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Details
- Title
- Identification of pyridazin-3-one derivatives as potent, selective histamine H-3 receptor inverse agonists with robust wake activity
- Creators
- Robert L. Hudkins - Cephalon Inc, Discovery Res, W Chester, PA 19380 USALisa D. Aimone - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAThomas R. Bailey - Cephalon Inc, Discovery Res, W Chester, PA 19380 USARobert J. Bendesky - 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 USAKurt A. Josef - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAYin-Guo Lin - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAJacquelyn Lyons - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAVal R. Marcy - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAJoanne R. Mathiasen - Cephalon Inc, Discovery Res, W Chester, PA 19380 USABabu G. Sundar - 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 USAEdward R. Bacon - Cephalon Inc, Discovery Res, W Chester, PA 19380 USA
- Publication Details
- Bioorganic & medicinal chemistry letters, v 21(18), pp 5493-5497
- Publisher
- Elsevier
- Number of pages
- 5
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000294051800075
- Scopus ID
- 2-s2.0-80051933140
- Other Identifier
- 991021900195104721
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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