References of "Pirotte, Bernard"
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See detailFrom the design to the clinical application of thromboxane modulators
Dogné, Jean-Michel ULg; Hanson, Julien ULg; de Leval, Xavier et al

in Current Pharmaceutical Design (2006), 12(8), 903-923

Arachidonic acid (AA) metabolites are key mediators involved in the pathogenesis of numerous cardiovascular, pulmonary, inflammatory, and thromboembolic diseases. One of these bioactive metabolites of ... [more ▼]

Arachidonic acid (AA) metabolites are key mediators involved in the pathogenesis of numerous cardiovascular, pulmonary, inflammatory, and thromboembolic diseases. One of these bioactive metabolites of particular importance is thromboxane A(2) (TXA(2)). It is produced by the action of thromboxane synthase on the prostaglandin endoperoxide H-2 (PGH(2)) which results from the enzymatic transformation of AA by the cyclooxygenases. It is a potent inducer of platelet aggregation, vasoconstriction and bronchoconstriction, and has been involved in a series of major pathophysiological conditions. Therefore, TXA(2) receptor antagonists, thromboxane synthase inhibitors and drugs combining both properties have been developed by different laboratories since the early 1980s. Several Compounds have been launched on the market and others are tinder clinical evaluation. In the first part of this review. we will describe the physiological properties of TXA(2), thromboxane synthase and thromboxane receptors. The second part is dedicated to a description of each class of thromboxane modulators with the advantages and disadvantages they offer. In the third part. we aim to describe recent studies performed with the most interesting thromboxane modulators in major pathologies: myocardial infarction and thrombosis, atherosclerosis, diabetes, pulmonary embolism, septic shock.. preeclampsia, and asthma. Each pathology will be systematically reviewed. Finally, in the last part we will highlight the latest perspectives in drug design of thromboxane modulators and in their future therapeutic applications such as cancer, metastasis and angiogenesis. [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 detailThe use of nimesulide and its analogues in cancer chemoprevention
Renard, Jean-François ULg; Julémont, F.; De Leval, X. et al

in Anti-Cancer Agents in Medicinal Chemistry (2006), 6

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See detailStructure-based pharmacophore of COX-2 selective inhibitors and identification of original lead compounds from 3D database searching method
Michaux, C.; De Leval, X.; Julémont, F. et al

in European Journal of Medicinal Chemistry (2006), 41

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See detailSynthesis and pharmacological evaluation of some N-arylsulfonyl-N-methyl-N'-(2,2-dimethyl-2-H-1-benzopyran-4-yl)ureas structurally related to cromakalim
Khelili, S.; Lebrun, P.; De Tullio, Pascal ULg et al

in Bioorganic & Medicinal Chemistry (2006), 14

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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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See detailBenzopyran derivatives, method of production and use thereof
Sebille, S.; Pirotte, Bernard ULg; Boverie, S. et al

Patent (2005)

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