References of "Pirotte, Bernard"
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See detailConception et synthèse d’outils pharmacologiques originaux pour l’étude des récepteurs au thromboxane
Moray, A. L.; Dogne, J. M.; Neven, P. et al

Poster (2007, May)

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See detailAChE Inhibitors and their Clinical Assessment
Francotte, Pierre ULg; De Tullio, Pascal ULg; Pirotte, Bernard ULg

in Protein Misfolding in Neurodegenerative Diseases: Mechanisms and Therapeutic Strategies (2007)

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See detailDesign, 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 ULg; De Tullio, Pascal ULg; Goffin, Eric ULg et al

in Journal of Medicinal Chemistry (2007), 50(13), 3153-3157

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 ... [more ▼]

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. [less ▲]

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See detailCholinergic Transmission and Acetylcholine release enhancers
Francotte, Pierre ULg; De Tullio, Pascal ULg; Pirotte, Bernard ULg

in Protein Misfolding in neuro degenerative Diseases : Mechanisms and Therapeutic Strategies (2007)

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See detailNovel dipyrazoles acting as glutamate modulators
Francotte, Pierre ULg; De Tullio, Pascal ULg; Pirotte, Bernard ULg

in Expert Opinion on Therapeutic Patents (2007), 17(12), 1489-1493

Knowing the potential therapeutic interest of AMPA potentiation, patents have been published for 15 years relating the discovery of novel compounds able to allosterically bind to the AMPA receptors and ... [more ▼]

Knowing the potential therapeutic interest of AMPA potentiation, patents have been published for 15 years relating the discovery of novel compounds able to allosterically bind to the AMPA receptors and leading to a potentiation of the AMPA signals. Besides this classical approach, a new target for the medicinal chemist has been defined due to the recent findings describing the modulation of AMPA receptors by neuronal proteins, and has led to the design of dipyrazole compounds by Aventis. These new dipyrazole derivatives may be considered as `indirect AMPApams', constituting a new pharmacological class. Based on their in vitro activity, it is probable that these compounds could be of therapeutic value for the treatment of cognitive disorders, schizophrenia or depression. [less ▲]

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See detailLaboratoire de Chimie pharmaceutique - ULg
Pirotte, Bernard ULg

in Chimie Nouvelle (2007), 95

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See detailPharmacological evaluation of TP receptor antagonists by differential activity on alpha and beta isoforms
Hanson, Julien ULg; Dogne, J. M.; Ghiotto, J. et al

Poster (2006, November 18)

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See detailNew developments in benzopyran derivatives as pancreatic β-cell KATP channel openers
Florence, X.; De Tullio, Pascal ULg; Lebrun, P. et al

Poster (2006, November 18)

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