Novel morpholine ketone analogs as potent histamine H-3 receptor inverse agonists with wake activity

[摘要]：Structure-activity relationship on a novel ketone class of H3R antagonists/inverse agonists is disclosed. Compound 4 showed excellent target potency, selectivity and brain penetration. Evaluation of antagonist 4 in the rat EEG/EMG model demonstrated robust wake activity thereby establishing preclinical proof of concept. (C) 2012 Elsevier Ltd. All rights reserved.

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