Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: Identification of candidates for clinical development

The pre-clinical characterization of novel aryloxypyridine amides that are histamine H-3 receptor antagonists is described. These compounds are high affinity histamine H-3 ligands that penetrate the CNS and occupy the histamine H-3 receptor in rat brain. Several compounds were extensively pro. led pre-clinically leading to the identification of two compounds suitable for nomination as development candidates. (C) 2010 Elsevier Ltd. All rights reserved.