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Pierre Fraikin
Researcher at University of Liège
Publications - 11
Citations - 321
Pierre Fraikin is an academic researcher from University of Liège. The author has contributed to research in topics: Benzothiadiazine & AMPA receptor. The author has an hindex of 10, co-authored 10 publications receiving 289 citations.
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Journal ArticleDOI
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†
Pierre Francotte,Pascal De Tullio,Eric Goffin,Gaëlle Dintilhac,E. Graindorge,Pierre Fraikin,Pierre Lestage,Laurence Danober,Jean-Yves Thomas,Daniel-Henri Caignard,Bernard Pirotte +10 more
TL;DR: The most potent compound, 4-ethyl-7-fluoro-3,4-dihydro-2H-1,2,4 -benzothiadiazine 1,1-dioxide was found to be active in an object recognition test in rats demonstrating cognition enhancing effects in vivo after oral administration.
Journal ArticleDOI
New fluorinated 1,2,4-benzothiadiazine 1,1-dioxides: discovery of an orally active cognitive enhancer acting through potentiation of the 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors.
Pierre Francotte,Eric Goffin,Pierre Fraikin,Pierre Lestage,Jean-Claude Van Heugen,Florian Gillotin,Laurence Danober,Jean-Yves Thomas,Patrice Chiap,Daniel-Henri Caignard,Bernard Pirotte,Pascal De Tullio +11 more
TL;DR: Results of this study clearly validated the positive impact of the fluorine atom on the alkyl chain at the 4-position of benzothiadiazine dioxides on activity and metabolic stability.
Journal Article
New trends in the design of drugs against Alzheimer's disease
TL;DR: This review presents an overview of the several strategies and new classes of compounds against AD and indicates some of these innovative approaches tend to delay onset of AD, while others are still symptomatic.
Journal ArticleDOI
In search of novel AMPA potentiators.
Pierre Francotte,Pascal De Tullio,Pierre Fraikin,Stéphane Counerotte,Eric Goffin,Bernard Pirotte +5 more
TL;DR: The enhancement of AMPA signals is an approach currently investigated for the management of Alzheimer's disease, schizophrenia or mood disorders and many efforts are being conducted in the development of AM PA positive allosteric modulators ("potentiators"), which alter the rate of receptor desensitization.
Journal ArticleDOI
Positive allosteric modulators of 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors belonging to 4-cyclopropyl-3,4-dihydro-2h-1,2,4-pyridothiadiazine dioxides and diversely chloro-substituted 4-cyclopropyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides.
Pierre Francotte,Ann-Beth Nørholm,Taru Deva,Lars Olsen,Karla Frydenvang,Eric Goffin,Pierre Fraikin,Pascal De Tullio,Sylvie Challal,Jean-Yves Thomas,Fabrice Iop,Caroline Louis,Iuliana Botez-Pop,Pierre Lestage,Laurence Danober,Jette S. Kastrup,Bernard Pirotte +16 more
TL;DR: Two 4-ethyl-substituted pyridothiadiazine dioxides belonging to α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor positive allosteric modulators were cocrystallized with the GluA2 ligand binding domain in order to decipher the impact of the position of the nitrogen atom on their binding mode at the AMPA receptors.