Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists.
Basic Information
ID: ALA1933007
Journal: Bioorg Med Chem Lett
Title: Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists.
Authors: Sundar BG, Bailey TR, Dunn DD, Bacon ER, Salvino JM, Morton GC, Aimone LD, Zeqi H, Mathiasen JR, Dicamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Brown R, Qian J, Angeles T, Connors T, Spais C, Holskin B, Galinis D, Duzic E, Schaffhauser H, Rosse GC.
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.
CiteXplore: 22153937
DOI: 10.1016/j.bmcl.2011.11.050
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