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Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 9, 2014, Pages 2079-2085

Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis

(13) Roecker, Anthony J a Mercer, Swati P a Harrell, C Meacham a Garson, Susan L a Fox, Steven V a Gotter, Anthony L a Prueksaritanont, Thomayant a Cabalu, Tamara D a Cui, Donghui a Lemaire, Wei a Winrow, Christopher J a Renger, John J a Coleman, Paul J a

a MERCK RESEARCH LABORATORIES (United States)

Author keywords

Antagonist; Bioactivation; Orexin; Pyrimidine; Sleep

Indexed keywords

2,4 DICHLOROPYRIMIDINE; ACETONITRILE; AMMONIUM HYDROXIDE; GLUTATHIONE; OREXIN 1 RECEPTOR; OREXIN 2 RECEPTOR; PYRIMIDINE DERIVATIVE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; ZINC; 2,4-DICHLOROPYRIMIDINE; OREXIN RECEPTOR;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DECHLORINATION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG SYNTHESIS; EXPERIMENTAL DOG; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; INSOMNIA; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PLASMA PROTEIN BINDING; RAT; REM SLEEP; SLEEP EFFICACY; SLEEP PARAMETERS; SLOW WAVE SLEEP; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECTS; SLEEP; SLEEP INITIATION AND MAINTENANCE DISORDERS; SYNTHESIS;

DORAS; RATTUS;

ANIMALS; DRUG DISCOVERY; HUMANS; OREXIN RECEPTORS; PYRIMIDINES; RATS; SLEEP; SLEEP INITIATION AND MAINTENANCE DISORDERS;

EID: 84899091110 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2014.03.052 Document Type: Article

Times cited : (11)

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