ORBi: Francotte Pierre - Design, synthesis, and pharmacology of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors

Reference : Design, synthesis, and pharmacology of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothi...


	Document type :	Scientific journals : Article
	Discipline(s) :	Human health sciences : Pharmacy, pharmacology & toxicology Physical, chemical, mathematical & earth Sciences : Chemistry
	To cite this reference:	http://hdl.handle.net/2268/6360

Title :	Design, synthesis, and pharmacology of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors
Language :	English
Author, co-author :	Francotte, Pierre [Université de Liège - ULg > > Chimie pharmaceutique >]
	De Tullio, Pascal [Université de Liège - ULg > > Chimie pharmaceutique >]
	Goffin, Eric [Université de Liège - ULg > > Chimie pharmaceutique >]
	Dintilhac, Gaëlle [Université de Liège - ULg > > Chimie pharmaceutique >]
	Graindorge, Emmanuel [> > > >]
	Fraikin, Pierre [Université de Liège - ULg > > Chimie pharmaceutique >]
	Lestage, Pierre [> > > >]
	Danober, Laurence [> > > >]
	Thomas, Jean-Yves [> > > >]
	Caignard, Daniel-Henri [> > > >]
	Pirotte, Bernard [Université de Liège - ULg > > Chimie pharmaceutique >]
Publication date :	2007
Journal title :	Journal of Medicinal Chemistry
Publisher :	Amer Chemical Soc
Volume :	50
Issue/season :	13
Pages :	3153-3157
Peer reviewed :	Yes (verified by ORBi)
Audience :	International
ISSN :	0022-2623
City :	Washington
Abstract :	[en] A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as potentiators of AMPA receptors. Attention was paid to the impact of the substituent introduced at the 7-position of the heterocycle. The biological evaluation was achieved by measuring the AMPA current in rat cortex mRNA-injected Xenopus oocytes. The most potent compound, 4-ethyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (12a) was found to be active in an object recognition test in rats demonstrating cognition enhancing effects in vivo after oral administration.
Target :	Researchers
Permalink :	http://hdl.handle.net/2268/6360

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