Article (Scientific journals)
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
Francotte, Pierre; De Tullio, Pascal; Goffin, Eric et al.
2007In Journal of Medicinal Chemistry, 50 (13), p. 3153-3157
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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.
Disciplines :
Chemistry
Pharmacy, pharmacology & toxicology
Author, co-author :
Francotte, Pierre  ;  Université de Liège - ULiège > Chimie pharmaceutique
De Tullio, Pascal ;  Université de Liège - ULiège > Chimie pharmaceutique
Goffin, Eric ;  Université de Liège - ULiège > Chimie pharmaceutique
Dintilhac, Gaëlle ;  Université de Liège - ULiège > Chimie pharmaceutique
Graindorge, Emmanuel
Fraikin, Pierre ;  Université de Liège - ULiège > Chimie pharmaceutique
Lestage, Pierre
Danober, Laurence
Thomas, Jean-Yves
Caignard, Daniel-Henri
Pirotte, Bernard ;  Université de Liège - ULiège > Chimie pharmaceutique
Language :
English
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
Publication date :
2007
Journal title :
Journal of Medicinal Chemistry
ISSN :
0022-2623
eISSN :
1520-4804
Publisher :
Amer Chemical Soc, Washington, United States - Washington
Volume :
50
Issue :
13
Pages :
3153-3157
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 16 February 2009

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