Wake-promoting agents: Search for next generation modafinil: Part IV

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. [Display omitted] N...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2012-08, Vol.54, p.949-951
Main Authors: Louvet, Philippe, Schweizer, Dominique, Gourdel, Marie-Edith, Riguet, Eric, Yue, Christoph, Marcy, Val R., Lin, Yin Guo, Gruner, John, Lesur, Brigitte, Bacon, Edward R., Chatterjee, Sankar
Format: Article
Language:English
Subjects:
Animals
Benzhydryl Compounds - chemistry
Benzhydryl Compounds - pharmacology
Biological and medical sciences
Cytochrome P-450 Enzyme Inhibitors
Diphenylether
Drug Discovery
Humans
Medical sciences
Miscellaneous
Modafinil
Pharmacology. Drug treatments
Rats
Wake-promoting agents
Wakefulness - drug effects
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Summary: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. [Display omitted] Novel compound 16 was conceptualized, synthesized and its enantiomers were characterized as a next generation molecule to modafinil (1), an atypical wake promoting agent. ► Ortho-diphenyl ether derived sulfinylacetamides are wake promoting agents (in rat). ► Para-analog of 3,4-dichloro ortho-derivative is less active in wake promotion assay. ► Enantiomers of 3,4-dichloro substituted ortho-analog differ in DAT binding assay.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2012.05.038