Referenced in: none

Automatically associated channels: Kv11.1

Title: Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists.

Authors: Babu G Sundar, Thomas R Bailey, Derek D Dunn, Edward R Bacon, Joseph M Salvino, George C Morton, Lisa D Aimone, Huang Zeqi, Joanne R Mathiasen, Amy Dicamillo, Mark J Huffman, Beth A McKenna, Karla Kopec, Lily D Lu, Rebecca Brown, Jie Qian, Thelma Angeles, Thomas Connors, Chrysanthe Spais, Beverly Holskin, Deborah Galinis, Emir Duzic, Hervé Schaffhauser, Gerard C Rosse

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 Jan 1 , 22, 120-3

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22153937

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.