Journal article
Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists
Bioorganic & medicinal chemistry letters, v 22(8), pp 2807-2810
15 Apr 2012
PMID: 22450133
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
Optimization of a series of aminomethyl ketone diamine H3R antagonists to reduce the brain exposure by lowering the pKa, led to molecules with improved pharmacokinetic properties. Compounds 9, 19, and 25 had high affinity for human H3R and demonstrated in vivo H3R functional activity in the rat dipsogenia model. Compound 9 displayed modest wake-promoting activity in the rat EEG/EMG model. (C) 2012 Elsevier Ltd. All rights reserved.
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Details
- Title
- Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists
- Creators
- Allison L. Zulli - Cephalon Inc, Discovery Res, W Chester, PA 19380 USALisa D. Aimone - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAJoanne R. Mathiasen - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAJohn A. Gruner - 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 USARobert L. Hudkins - Cephalon Inc, Discovery Res, W Chester, PA 19380 USA
- Publication Details
- Bioorganic & medicinal chemistry letters, v 22(8), pp 2807-2810
- Publisher
- Elsevier
- Number of pages
- 4
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000302768200035
- Scopus ID
- 2-s2.0-84859438207
- Other Identifier
- 991021900191604721
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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