1.
Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity.
Bioorg Med Chem Lett
; 22(4): 1546-9, 2012 Feb 15.
Article
in English
| MEDLINE
| ID: mdl-22297111
ABSTRACT
Structure-activity relationship on a novel ketone class of H(3)R 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.
