Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists

Babu G. Sundar, T. R. Bailey,Derek Dunn,Edward R. Bacon,Joseph M. Salvino, George Morton,Lisa D. Aimone,Zeqi Huang,Joanne R. Mathiasen, Amy DiCamillo, Mark J. Huffman, Beth Ann McKenna,Karla Kopec, Lily Lu,Rebecca S. Brown,Jie Qian,Thelma S. Angeles, T. A. Connors,Chrysanthe Spais,Beverly P. Holskin, Deborah L. Galinis,Emir Duzic,Hervé Schaffhauser,Gérard Rossé

Bioorganic & Medicinal Chemistry Letters（2012）

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摘要

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.

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novel brain penetrant benzofuropiperidine,receptor

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