Bioorganic & Medicinal Chemistry Letters 2010-11-01

Investigation of 4-piperidinols as novel H3 antagonists.

James T Anderson, Michael Campbell, Jianmin Wang, Kurt R Brunden, John J Harrington, Alain Stricker-Krongrad, Jianping Song, Chris Doucette, Steven Murphy, Youssef L Bennani

Index: Bioorg. Med. Chem. Lett. 20(21) , 6246-9, (2010)

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Abstract

Compounds containing a substituted 4-piperidinol core have been found to be potent antagonists of the human H(3) receptor. The compounds exhibited up to a 60-fold preference for inhibiting the human H(3) receptor over the mouse and showed a low binding affinity for the hERG channel.Copyright © 2010 Elsevier Ltd. All rights reserved.