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Peer Reviewed
See detailDesign, synthesis and biological evaluation of sulfonylureas as original non-prostanoïd thromboxane A2 receptor antagonists
Dogne, J. M.; De Leval, X.; Damas, J. et al

Conference (1998, November 27)

Detailed reference viewed: 6 (0 ULg)
Peer Reviewed
See detailDesign, synthesis and biological evaluation of sulfonylureas as original non-prostanoid thromboxane A2 receptor antagonists
Dogne, J. M.; De Leval, X.; Damas, J. et al

Poster (1998, November 27)

Detailed reference viewed: 18 (0 ULg)
Peer Reviewed
See detailDesign, synthesis and biological evaluation of sulfonylureas as original non-prostanoid thromboxane receptor antagonists
Dogne, J. M.; Varache-Lembege, M.; Damas, J. et al

Conference (1997, April)

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See detailDesign, synthesis and evaluation of graftable thrombin inhibitors for the preparation of blood-compatible polymer materials.
Salvagnini, Claudio; Michaux, Catherine; Remiche, Julie ULg et al

in Organic & Biomolecular Chemistry (2005), 3(23), 4209-20

Piperazinyl-amide derivatives of N-alpha-(3-trifluoromethyl-benzenesulfonyl)-L-arginine (1) were synthesized as graftable thrombin inhibitors. The possible disturbance of biological activity due to a ... [more ▼]

Piperazinyl-amide derivatives of N-alpha-(3-trifluoromethyl-benzenesulfonyl)-L-arginine (1) were synthesized as graftable thrombin inhibitors. The possible disturbance of biological activity due to a variable spacer-arm fixed on the N-4 piperazinyl position was evaluated in vitro, against human alpha-thrombin, and in blood coagulation assay. Molecular modelling (in silico analysis) and X-ray diffraction studies of thrombin-inhibitor complexes were also performed. The fixation of bioactive molecules on poly(butylene terephthalate) (PBT) and poly(ethylene terephthalate) (PET) membranes was performed by wet chemistry treatment and evaluated by XPS analysis. Surface grafting of inhibitor 1d improved the membrane hemocompatibility by reducing blood clot formation on the modified surface. [less ▲]

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See detailDesign, synthesis and pharmacological evaluation of dimeric ligands for the benzothiadiazine dioxide allosteric binding site of the AMPA receptors
Drapier, Thomas ULg; Francotte, Pierre ULg; Pirotte, Bernard ULg et al

Conference (2015, June 04)

L-glutamic acid is the major excitatory neurotransmitter in the brain. It exerts its effects through metabotropic and ionotropic receptors. Among the latter, three subtypes have been identified: NMDA ... [more ▼]

L-glutamic acid is the major excitatory neurotransmitter in the brain. It exerts its effects through metabotropic and ionotropic receptors. Among the latter, three subtypes have been identified: NMDA, AMPA and KA receptors. It is now well established that a deficit in glutamatergic signaling may be responsible for neurological disorders such as schizophrenia, depression, mild cognitive impairment and ADHD. Enhancement of the signal through positive allosteric modulators of AMPA receptors might be a therapeutic issue for these diseases. These compounds are expected to exert a fine tuning of the signal. Since they require the presence of the endogenous ligand to be active, they are expected to induce less toxicity than agonists. In this context, based on the structure of known allosteric modulators of AMPA receptors such as cyclothiazide (1) and IDRA 21 (2), the Laboratory of Medicinal Chemistry (University of Liège) has developed a series of 1,2,4-benzothiadiazine 1,1-dioxides with high potency as AMPA receptor potentiators, among which compounds (3) and (4). Crystallographic data obtained by the Department of Medicinal Chemistry (University of Copenhagen) highlighted that (3) and (4) bind to two contiguous sites at the dimer interface of the ligand binding domain of the AMPA receptor1,2. From these data, we may expect that the synthesis of dimeric molecules could lead to further improvement in affinity and activity. Our work consists in the development of a family of dimeric benzothiadiazine dioxides and their evaluation in a pharmacological assay. Several structural parameters such as the position of the bridge on the aromatic ring between the two heterocycles as well as its nature and length will be studied in order to determine their impact on the activity and thus the affinity. [less ▲]

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See detailDesign, synthesis and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors
Julémont, F.; de Leval, X.; Michaux, C. et al

in Journal of Medicinal Chemistry (2004), 47

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See detailDesign, synthesis and pharmacological evaluation of sulfonylureas and sulfonycyanoguanidines as thromboxane A2 receptor antagonists. Insights into selectivity between thromboxane A2 receptor isoforms (TPα et TPβ)
Hanson, Julien ULg

Doctoral thesis (2007)

Thromboxane A2 (TXA2) is an important mediator metabolized from arachidonic acid through the cyclooxygenase pathway, mainly in platelets and macrophages. It is a potent inducer of platelet aggregation and ... [more ▼]

Thromboxane A2 (TXA2) is an important mediator metabolized from arachidonic acid through the cyclooxygenase pathway, mainly in platelets and macrophages. It is a potent inducer of platelet aggregation and smooth muscle contraction. Its overproduction has been detected in pathologies such as stroke, asthma, myocardial infarction or atherosclerosis. The action of TXA2 is mediated by a specific G-protein coupled receptor (TP) of which two alternative spliced isoforms, TPalpha and TPbeta, have been described. The exact role of these two isoforms is not clearly understood. However, recent studies have described their implications in vascular physiology and pathology. The inhibition of the action of TXA2 on platelets and blood vessels would be interesting as original therapies against cardiovascular diseases. Consequently, the design of TP receptor antagonists remains of great interest in cardiovascular medicine. In the laboratory of medicinal chemistry (University of Liège, Belgium), several nitrobenzenesulfonylureas, derived from torasemide (a loop diuretic), have been previously described as TP receptor antagonists. Two compounds, BM573 and BM613 were among the most interesting molecules identified in that previous work. The present project is divided in two parts. First, we have determined the pharmacological properties of BM573 and BM613 as thromboxane synthase inhibitors and TP receptor antagonists, in vitro and in vivo. In our assays, these two compounds were proved to have high affinity for both TPalpha and TPbeta, to be potent antiplatelet agents, to inhibit thromboxane synthase and TP-mediated smooth muscle contraction. Additionally, they significantly reduced the size of the thrombus in a rat model of ferric chloride-induced arterial thrombosis. Consequently, we demonstrated that the TP receptor antagonists BM573 and BM613, belonging to the chemical family of nitrobenzenesulfonylureas, could be regarded as antiplatelet and antithrombotic agents potentially useful in thromboxane-related diseases such as stroke or myocardial infarction. Secondly, given the interesting pharmacological profile of BM573 and BM613, we have designed and synthesized several series of compounds derived from these two agents. We have evaluated the binding properties (affinity) of the first generation (+/- 35 original derivatives) of compounds on either TPalpha or TPbeta, transiently expressed in COS-7 cell lines. Additionally, we have measured the ability of our drugs to inhibit the intracellular calcium mobilization upon TPalpha or TPbeta stimulation. To confirm our results, we also assessed the antiplatelet properties of our drugs by means of determination of inhibition of human platelet aggregation. On the basis of the results obtained with these in vitro assays, we have synthesized and evaluated a second generation of derivatives (+/- 35 original compounds) and improved the selectivity of several original compounds for TP receptor isoforms. The originality of this work was to evaluate a large library of synthetic compounds on both TP receptor isoforms, using specific pharmacological tests. By means of structure-activity relationship studies, we were able to identify chemical groups implicated in selectivity and to propose lead compounds for development of highly specific TPalpha or TPbeta antagonists. Besides, we have identified an in vivo drug candidates for prevention of thrombosis and pathological platelet aggregation. [less ▲]

Detailed reference viewed: 40 (13 ULg)
Peer Reviewed
See detailDesign, synthesis and pharmacology of sulfonylcyanoguanidines and sulfonamidonitroethylenes as bioisosteres of hypoglycemic sulfonylureas
Masereel, B.; Ouedraogo, R.; Dogne, J. M. et al

Poster (1997, May)

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Peer Reviewed
See detailDesign, synthesis and pharmacology of sulfonylcyanoguanidines and sulfonamidonitroethylenes as bioisosteres of hypoglycemic sulfonylureas
Masereel, B.; Ouedraogo, R.; Dogne, J.-M. et al

in Journal de Pharmacie de Belgique (1998), 53

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Peer Reviewed
See detailDesign, synthesis, and pharmacological evaluation of cromakalim analogues as pancreatic β-cell-selective KATP channel openers
Florence, X.; De Tullio, Pascal ULg; Lebrun, Ph. et al

Conference (2007, October)

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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 detailLes désignations de plats étrangères dans le Cuisnier gascon (1740)
Colson, Maryse ULg

Conference (2011, May 13)

Œuvre originale de la première moitié du XVIIIe siècle, Le Cuisinier gascon est certainement l’un des ouvrages culinaires les plus énigmatiques de son époque. Publié de façon anonyme, le livre est ... [more ▼]

Œuvre originale de la première moitié du XVIIIe siècle, Le Cuisinier gascon est certainement l’un des ouvrages culinaires les plus énigmatiques de son époque. Publié de façon anonyme, le livre est aujourd’hui attribué au Prince de Dombes, frère du comte d’Eu et grand veneur de Louis XV avec lequel il partage le goût de la chasse et des bons repas. L’ouvrage présente deux cent dix-sept recettes disparates dont l’écriture ne déroge à aucune règle fondamentale : concision et efficacité du style, sobriété de la syntaxe, homogénéité des moyens d’expression de l’injonction. En effet, la recette de cuisine, par sa nature prescriptive, laisse peu de place aux figures stylistiques et à la créativité de son auteur. En réalité, le seul espace qui permet de laisser quelque latitude à l’imagination est concentré dans l’intitulé du plat décrit. Or, Le Cuisinier gascon présente de nombreuses désignations de plats fantaisistes et, en particulier, un nombre impressionnant de dénominations « étrangères » telles que les Cuisses de poularde à la Suisse ou les Poulpettes à l’Italienne. Il est donc évident que l’ouvrage se veut cosmopolite, résolument tourné vers l’ailleurs – qu’il soit géographique ou imaginaire. De manière générale, nous nous demanderons dans quelle mesure les emprunts lexicaux tels que Woatre fiche, oille et niocs peuvent être considérés comme des transferts culturels, à la fois matériel (la spécialité culinaire) et linguistique (sa dénomination). Peut-on voir dans cet exotisme culinaire le signe d’influences culturelles entre des pays dont les frontières politiques ne cessent de se redessiner durant un siècle éclairé par les Lumières ? En particulier, deux types de désignations problématiques retiendront notre attention ; le premier type portant sur « l’ailleurs spatial » et le second sur « l’ailleurs imaginaire ». Premièrement, on note de nombreux adjectifs invariables construits sur le modèle « à la + adj. fém. sg. » : les uns réfèrent à des régions (à la Provençale) et les autres à des entités culturelles plus vastes (à l’Espagnole). Si le lien entre la désignation et la référence est parfois évident (par exemple, on trouve presque invariablement du parmesan dans la composition des plats à l’Italienne), il peut s’avérer abscons dans d’autres cas ; ainsi, nous rencontrons des Choux à la Turque et des Foyes gras à l’Indienne qui n’ont rien d’oriental. Ces qualifications sont-elles purement fantaisistes ou ont-elles une explication rationnelle ? Ces adjectifs font-il véritablement référence à une nation ou plutôt à une tradition, à un événement historique ou à une personnalité ? Deuxièmement, on observe des désignations inédites, propres au Cuisinier gascon : les Yeux de veau farcis au gratin, le Hachis d’œufs sans malice et le Veau en crotte d’âne roulé à la Nenteau en sont les meilleurs exemples. Ici, ce ne sont plus les frontières géographiques qui sont franchies, mais celles du réel. Comment comprendre l’étrangeté de ces appellations qui mêlent la représentation imagée des aliments et une poésie pleine d’humour ? Ne pourrait-on lire dans cette liberté nominative la volonté de l’auteur-cuisinier de s’émanciper en s’appropriant la matière culinaire grâce à l’usage qu’il fait de la langue ? Par l’étude de quelques désignations, nous verrons à quel point les transferts culturels imprègnent la gastronomie de l’époque et lui permettent d’évoluer. De plus, nous envisagerons la possibilité que le cuisinier, en introduisant l’étrange ou l’étranger dans son texte, devienne lui-même autre (un véritable auteur) et qu’il emmène le genre culinaire vers un ailleurs: la gasconnade. [less ▲]

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See detailLes désignations romanes de l'ECUREUIL
Boutier, Marie-Guy ULg; Baiwir, Esther ULg

in Contini, Michel; Veny, Joan (Eds.) Atlas linguistique roman (ALiR) (in press)

L'ALiR a pour objectif de fournir une description globale du lexique roman par champ sémantique, à travers l'étude onomasiologique des désignations romanes de concepts. Les analyses lexicale, phonétique ... [more ▼]

L'ALiR a pour objectif de fournir une description globale du lexique roman par champ sémantique, à travers l'étude onomasiologique des désignations romanes de concepts. Les analyses lexicale, phonétique, morphosyntaxiques sont mises en valeur par la production de cartes interprétatives. [less ▲]

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See detailDesigned combination of chiral selectors for adjustment of enantioseparation selectivity in capillary electrophoresis.
Fillet, Marianne ULg; Chankvetadze, Bezhan; Crommen, Jacques ULg et al

in Electrophoresis (1999), 20(13), 2691-7

In this study an attempt has been made to explain the reasons for changing the enantioseparation selectivity in some dual cyclodextrin (CD) systems compared to the use of single chiral selectors in ... [more ▼]

In this study an attempt has been made to explain the reasons for changing the enantioseparation selectivity in some dual cyclodextrin (CD) systems compared to the use of single chiral selectors in capillary electrophoresis (CE). An explanation for selectivity changes is proposed based on the effect of the chiral selector on the mobility of the analyte. In order to support the proposed mechanism, several dual systems were designed on the basis of the known recognition pattern of enantiomers for individual CDs. In most cases the separation selectivity could be adjusted in a designed way. There was no experimental evidence for simultaneous binding of a given chiral analyte with both chiral selectors or of chiral recognition of an analyte complex with one CD by another CD. [less ▲]

Detailed reference viewed: 70 (2 ULg)