Journal article
Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists
Bioorganic & medicinal chemistry letters, v 22(1), pp 120-123
01 Jan 2012
PMID: 22153937
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel scaffold for 5HT(6) receptor antagonists. Optimization by substitution at C-1 position led to identification of selective, orally bioavailable, brain penetrant antagonists with reduced hERG liability. An advanced analog tested in rat social recognition model showed significant activity suggesting potential utility in the enhancement of short-term memory. (C) 2011 Elsevier Ltd. All rights reserved.
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Details
- Title
- Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists
- Creators
- Babu G. Sundar - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAThomas R. Bailey - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USADerek D. Dunn - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAEdward R. Bacon - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAJoseph M. Salvino - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAGeorge C. Morton - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USALisa D. Aimone - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAHuang Zeqi - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAJoanne R. Mathiasen - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAAmy Dicamillo - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAMark J. Huffman - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USABeth A. McKenna - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAKarla Kopec - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USALily D. Lu - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USARebecca Brown - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAJie Qian - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAThelma Angeles - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAThomas Connors - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAChrysanthe Spais - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USABeverly Holskin - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USADeborah Galinis - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAEmir Duzic - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAHerve Schaffhauser - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USAGerard C. Rosse - Cephalon Inc, Worldwide Discovery Res, W Chester, PA 19380 USA
- Publication Details
- Bioorganic & medicinal chemistry letters, v 22(1), pp 120-123
- Publisher
- Elsevier
- Number of pages
- 4
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000298636700018
- Scopus ID
- 2-s2.0-84655176422
- Other Identifier
- 991021900193104721
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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