References of "Pirotte, Bernard"
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See detailOriginal cromakalim analogues as KATP channel openers
Florence, Xavier ULg; De Tullio, Pascal ULg; Pirotte, Bernard ULg et al

in Metabolic and Functional Research on Diabetes (2009), 2

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See detail6-Substituted 2-Oxo-2h-1-Benzopyran-3-Carboxylic Acid Derivatives in a New Approach of the Treatment of Cancer Cell Invasion and Metastasis
Kempen, I.; Hemmer, Marc ULg; Counerotte, Stéphane ULg et al

in European Journal of Medicinal Chemistry (2008), 43(12), 2735-50

Novel 6-substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives were synthesized and their potency in reducing the invasive behaviour of HT 1080 fibrosarcoma cells was evaluated. Structure ... [more ▼]

Novel 6-substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives were synthesized and their potency in reducing the invasive behaviour of HT 1080 fibrosarcoma cells was evaluated. Structure-activity relationships were deduced from biological results and will be used in further design of new active compounds. In particular, the acetoxymethyl substituent found at the 6-position of previously described active compounds can be replaced by an acetamidomethyl substituent without loss of potency; while the presence of an aryl ester function at the 3-position was preferred to a thioester or an amide function to induce marked biological activity. This work confirms the interest of aryl esters of 6-substituted coumarin-3-carboxylic acids as potential new anti-cancer agents. [less ▲]

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See detail1H NMR metabolomic approach of the laser-induced choroidal neovascularization in mice
Lambert, Vincent ULg; Frederich, Michel ULg; Rousseau, Rousseau et al

Poster (2008, August)

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See detail6-Substituted benzopyran derivatives as potent KATP channel openers: synthesis and biological in vitro evaluation
Florence, X.; De Tullio, Pascal ULg; Lebrun, P. et al

Poster (2008, May)

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See detailInhibitory effect of curcuminoids and tetrahydrocurcuminoids on equine activated neutrophils and myeloperoxidase activity
Franck, Thierry ULg; Kohnen, Stephan ULg; Grulke, Sigrid ULg et al

in Physiological Research (2008), 57(4), 577-587

In the horse, the inflammation response to various pathologies (intestinal strangulations, laminitis, etc.) involves an excessive stimulation of the polymorphonuclear neutrophils releasing reactive oxygen ... [more ▼]

In the horse, the inflammation response to various pathologies (intestinal strangulations, laminitis, etc.) involves an excessive stimulation of the polymorphonuclear neutrophils releasing reactive oxygen species (ROS) and myeloperoxidase (MPO). The aim of the present work was to study the effect of natural polyphenols, curcuminoids and tetrahydrocurcuminoids (THC) on isolated stimulated equine neutrophils and on the activity of purified MPO. The ROS production and the release of MPO by activated neutrophils were measured by chemiluminescence and ELISA techniques, respectively. The activity of purified MPO was measured by studying its nitration, chlorination or oxidation capacity and by using an original method called SIEFED allowing the study of drug interaction with the enzyme without interferences of the medium. Curcuminoids and THC had dose-dependent inhibitory effects on ROS production and MPO release by activated neutrophils and on purified MPO activity. We suggest that the higher efficacy of curcuminoids versus THC could be explained, at least partially, by its chemical structure: the conjugated double bounds and the plane structure of curcuminoids made easier the neutralization of the radical species generated by activated neutrophils and the interaction of the drug with the active site of MPO. These inhibitory effects of curcuminoids on the oxidant activity of equine neutrophils and on MPO activity open therapeutic perspectives in equine pathologies with excessive inflammatory reactions. [less ▲]

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See detailTowards the control of intercellular protein turnover: Mitochondrial Lon protease inhibitors versus proteasome inhibitors
Bayot, A.; Basse, N.; Lee, I. et al

in Biochimie (2008), 90

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See detailKATP channel openers: tissue selectivity of original 3-alkylaminopyrido- and 3-alkylaminobenzothiadiazine 1,1 -dioxides
Lebrun, P.; Becker, B.; Morel, N. et al

in Biochemical Pharmacology (2008), 75

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See detailSynthesis and activity on rat aorta rings and rat pancreatic beta-cells of ring-opened analogues of benzopyran-type potassium channel activators
Khelili, S.; Florence, Xavier ULg; Bouhadja, M. et al

in Bioorganic & Medicinal Chemistry (2008), 16

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See detailSynthesis and pharmacological evaluation of a second generation of pyridothiadiazine 1,1-dioxides acting as AMPA potentiators.
Francotte, Pierre ULg; De Tullio, Pascal ULg; Podona, Tchao et al

in Bioorganic & Medicinal Chemistry (2008), 16(23), 9948-56

Taking into account structure-activity relationships obtained with our previous series, new diversely substituted 1,2,4-pyridothiadiazine 1,1-dioxides were designed to obtain novel AMPA potentiators. The ... [more ▼]

Taking into account structure-activity relationships obtained with our previous series, new diversely substituted 1,2,4-pyridothiadiazine 1,1-dioxides were designed to obtain novel AMPA potentiators. The aim of this work was focused on the improvement of lipophilicity, which is well known as a critical parameter to obtain in vivo active central nervous system agents. For this purpose, two positions on the pyridine ring were privileged to insert selected groups. Among the synthesized compounds emerged 7-chloro-4-ethyl-3,4-dihydro-2H-pyrido[2,3-e]-[1,2,4]-thiadiazine 1,1-dioxide (12d), which was evaluated in two memory tests in Wistar rats and showed cognition enhancing effects after intraperitoneal injection at doses as low as 0.3mg/kg. [less ▲]

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See detailNew pyridinic analogues of nimesulide as potent COXs inhibitors.
Renard, Jean-François ULg; Garbacki, Nancy ULg; de Leval, Xavier et al

Poster (2008)

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See detailDevelopment of original pyridinic analogues of nimesulide as cycloxygenase inhibitors
Renard, Jean-François ULg; de Leval, Xavier; Pirotte, Bernard ULg

Conference (2007, October)

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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 detailThrombin activity profile: a rapid, reliable and relevant ex vivo screening test for the development of anticoagulant drugs
Robert, S.; Ghiotto, J.; Pirotte, Bernard ULg et al

Conference (2007, October)

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See detailDesign, synthesis and anticancer activity of novel hydroxylated coumarin derivatives
Hemmer, Marc ULg; De Tullio, Pascal ULg; Bernard, Y. et al

Conference (2007, October)

Detailed reference viewed: 18 (0 ULg)