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Bioorg Med Chem Lett. 2012 Jan 1;22(1):120-3. doi: 10.1016/j.bmcl.2011.11.050. Epub 2011 Nov 22.

Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists.

Author information

1
Worldwide Discovery Research, Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380, USA. bsundar@cephalon.com

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.

PMID:
22153937
DOI:
10.1016/j.bmcl.2011.11.050
[Indexed for MEDLINE]

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