Reference : Design, synthesis, and pharmacology of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothi...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
Physical, chemical, mathematical & earth Sciences : Chemistry
http://hdl.handle.net/2268/6360
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
English
Francotte, Pierre mailto [Université de Liège - ULg > > Chimie pharmaceutique >]
De Tullio, Pascal mailto [Université de Liège - ULg > > Chimie pharmaceutique >]
Goffin, Eric mailto [Université de Liège - ULg > > Chimie pharmaceutique >]
Dintilhac, Gaëlle mailto [Université de Liège - ULg > > Chimie pharmaceutique >]
Graindorge, Emmanuel [> > > >]
Fraikin, Pierre mailto [Université de Liège - ULg > > Chimie pharmaceutique >]
Lestage, Pierre [> > > >]
Danober, Laurence [> > > >]
Thomas, Jean-Yves [> > > >]
Caignard, Daniel-Henri [> > > >]
Pirotte, Bernard mailto [Université de Liège - ULg > > Chimie pharmaceutique >]
2007
Journal of Medicinal Chemistry
Amer Chemical Soc
50
13
3153-3157
Yes (verified by ORBi)
International
0022-2623
Washington
[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.
Researchers
http://hdl.handle.net/2268/6360

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