References of "Francotte, Pierre"
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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 detailNew trends in the design of drugs against Alzheimer's disease
Francotte, Pierre ULg; De Tullio, Pascal ULg; Fraikin, Pierre ULg et al

in Frontiers in Medicinal Chemistry (2006), 3

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See detailIn Search of Novel Ampa Potentiators
Francotte, Pierre ULg; De Tullio, Pascal ULg; Fraikin, Pierre ULg et al

in Recent Patents on CNS Drug Discovery (2006), 1(3), 239-46

Glutamate is the major excitatory neurotransmitter in the brain. Amongst ionotropic receptors responding to glutamate, the AMPA subtype has been considered as essential for the fast excitatory ... [more ▼]

Glutamate is the major excitatory neurotransmitter in the brain. Amongst ionotropic receptors responding to glutamate, the AMPA subtype has been considered as essential for the fast excitatory neurotransmission in the central nervous system and the expression and maintenance of long-term potentiation. As glutamate is known to be involved in many neurological and psychiatric disorders, AMPA receptors seem to represent interesting targets to develop therapeutic drugs. Hence, the enhancement of AMPA signals is an approach currently investigated for the management of Alzheimer's disease, schizophrenia or mood disorders. In particular, many efforts are being conducted in the development of AMPA positive allosteric modulators ("potentiators"), which alter the rate of receptor desensitization. The major chemical families developed as AMPA potentiators are aniracetam derivatives, cyclothiazide derivatives and biarylpropylsulfonamides derivatives. [less ▲]

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