Design, synthesis and pharmacological evaluation of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides acting as AMPA potentiators

Poster (2008, May 17)

Design, synthesis and pharmacological evaluation of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides acting as AMPA potentiators

Poster (2006, August)

Preparation of 5-(1,1'-biphenyl)-4-yl-5-(4-(4-aminoacylphenyl)-piperazin)-1-yl-pyrimidine-2,4,6-triones and their use as inhibitors of zinc metalloendopeptidases

Patent (2006)

In Search of Novel Ampa Potentiators

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 ▲]

3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers : effect of 6,7-distribution on potency and tissue selectivity

in Journal of Medicinal Chemistry (2005), 48

Effects of recently developed 6-substituted 3-bromophenyl 2-oxo-2H-1-benzopyran-3-carboxylate derivatives on HT1080 cell invasion in vitro

Poster (2003, November 22)

3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo

in British Journal of Cancer (2003), 88(7), 1111-1118

In search for new anticancer agents, we have evaluated the antiinvasive and antimigrative properties of recently developed synthetic coumarin derivatives among which two compounds revealed important ... [more ▼]

In search for new anticancer agents, we have evaluated the antiinvasive and antimigrative properties of recently developed synthetic coumarin derivatives among which two compounds revealed important activity: 3-chlorophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate and 3-bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate, Both drugs were able to inhibit cell invasion markedly in a Boyden chamber assay, the bromo derivative being more potent than the reference matrix metalloprotease (MMP) inhibitor GI 129471. In vivo, tumour growth was reduced when nude mice grafted with HT 1080 or MDA-MB231 cells were treated i.p. 3 days week(-1) with the bromo coumarin derivative. These effects were not associated with the inhibition of urokinase, plasmin, MMP-2 or MMP-9. The mechanism of action of the drugs remains to be elucidated. However, these two coumarin derivatives may serve as new lead compounds of an original class of antitumour agents. [less ▲]

Les esters du 6-hydroxyméthyl-2-oxo-2H-1-benzopyrane-3-carboxylate de 3-bromophényle en tant qu’agents inhibiteurs de l’invasion cellulaire in vitro

Poster (2002, May)

Effects on in vitro and in vivo cellular invasion of two 6-(acetoxymethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives

Poster (2001, October 16)

Effects on cellular invasion of two synthetic coumarins

Conference (2001, May)