Thrombin activity profile : a powerful ex vivo screening test for the development of anticoagulant drugs

Poster (2007, July)

Le profil d’activité de thrombine: un puissant test de criblage ex vivo pour le développement d’agents anticoagulants

Poster (2007, May)

Conception, synthèse et évaluation biologique de composés coumariniques en tant qu’agents anti-cancéreux potentiels

Poster (2007, May)

Synthèse et évaluation biologique de nouveaux activateurs des canaux potassiques ATP-dépendants en série benzopyrane

Poster (2007, May)

Coupling of the LC-MS/MS and the LC-SPE-NMR for the structural identification of pancreatic KATP channel openers metabolites following in vitro biotransformation

Poster (2007)

AChE Inhibitors and their Clinical Assessment

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

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

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 ▲]

Novel dipyrazoles acting as glutamate modulators

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 ▲]

Etude de la métabolisation in vitro d’activateurs des canaux potassiques appurtenant à la classe des 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxydes: utilisation conjuguée de la LC-MS et de la LC-SPE-NMR

Scientific conference (2006, December 14)

Pharmacological evaluation of TP receptor antagonists by differential activity on alpha and beta isoforms

Poster (2006, November 18)