1.
Eur J Med Chem
; 54: 949-51, 2012 Aug.
Article
in English
| MEDLINE
| ID: mdl-22749190
ABSTRACT
In search of a next generation molecule to the novel wake promoting agent modafinil, a series of diphenyl ether derived wakefulness enhancing agents (in rat) was developed. From this work, racemic compound 16 was separated into its chiral enantiomers to profile them individually.
Subject(s)
Benzhydryl Compounds/pharmacology , Wakefulness/drug effects , Animals , Benzhydryl Compounds/chemistry , Cytochrome P-450 Enzyme Inhibitors , Drug Discovery , Humans , Modafinil , Rats
2.
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.
