References of "Pirotte, Bernard"
     in
Bookmark and Share    
Peer Reviewed
See detailDevelopment of thromboxane A2 modulators as promising anti-metastatic and anti-angiogenic compounds
De Leval, X.; Dassesse, T.; Benoit, V. et al

Conference (2004, May)

Detailed reference viewed: 2 (0 ULg)
Full Text
Peer Reviewed
See detailNew developments on thromboxane modulators
Dogné, Jean-Michel ULg; Hanson, Julien ULg; De leval, X. et al

in Mini Reviews in Medicinal Chemistry (2004)

Detailed reference viewed: 18 (3 ULg)
Full Text
Peer Reviewed
See detailEffects of COX-2 inhibitors on ROS produced by Chlamydia pneumoniae-primed human promonocytic cells (THP-1)
Mouithys-Mickalad, Ange ULg; Deby, Ginette ULg; Dogné, Jean-Michel ULg et al

in Biochemical and Biophysical Research Communications (2004), 325(4), 1122-1130

Chronic inflammation through foam cells and macrophages is important in atherosclerosis development, and can be considered as therapeutic targets. Cyclooxygenase and NADPH-oxidase were expressed within ... [more ▼]

Chronic inflammation through foam cells and macrophages is important in atherosclerosis development, and can be considered as therapeutic targets. Cyclooxygenase and NADPH-oxidase were expressed within atherosclerotic lesions. Reactive oxygen species produced by NADPH oxidase were found to trigger the cyclooxygenase-2 expression. The effects of preferential COX-2 inhibitors on ROS produced by Chlamydia-primed human monocytes (THP-1 cells) were evaluated by fluorescence, chemiluminescence, oxymetry, and EPR spin trapping. Fluorescence assays showed an increased production of ROS with Chlamydia versus cells primed by 10(-8) M PMA. COX-2 inhibitors inhibited in a dose-dependent manner the luminol-enhanced CL while ibuprofen and diclofenac increased the chemiluminescence response. By EPR spin trapping, COX-2 inhibitors, ibuprofen, and diclofenac, exhibited a dose-dependent inhibiting effect (10 and 100 muM) on the EPR signal appearance. Our cell model combining EPR, chemiluminescence, and oxymetry appeared relevant to study the modulating effects of preferential COX-2 inhibitors on the cell oxidant activity and chronic inflammatory diseases. (C) 2004 Elsevier Inc. All rights reserved. [less ▲]

Detailed reference viewed: 121 (36 ULg)
Full Text
Peer Reviewed
See detailNew developments on thromboxane and prostacyclin modulators. Part II: prostacyclin modulators
De Leval, X.; Hanson, Julien ULg; David, Jean-Louis ULg et al

in Current Medicinal Chemistry (2004), 11

Detailed reference viewed: 19 (1 ULg)
Full Text
Peer Reviewed
See detailFirst and second generations of COX-2 selective inhibitors
De leval, X.; Julémont, F.; Benoit, V. et al

in Mini Reviews in Medicinal Chemistry (2004), 4

Detailed reference viewed: 22 (4 ULg)
Full Text
Peer Reviewed
See detailRecent developments in the chemistry of potassium channel activators : the cromakalim analogues
Sebille, S.; De Tullio, Pascal ULg; Boverie, S. et al

in Current Medicinal Chemistry (2004), 11

Detailed reference viewed: 11 (0 ULg)
Full Text
Peer Reviewed
See detailCharacterization of preferential activity on platelet thromboxane A2 receptors of BM-613, a new thromboxane A2 antagonist
Hanson, Julien ULg; Rolin, S.; De Leval, X. et al

in Fundamental & Clinical Pharmacology (2004)

Detailed reference viewed: 3 (1 ULg)
Full Text
Peer Reviewed
See detailNew developments on thromboxane and prostacyclin modulators. Part I: thromboxane modulators
Dogné, Jean-Michel ULg; De leval, X.; Hanson, Julien ULg et al

in Current Medicinal Chemistry (2004), 11

Detailed reference viewed: 21 (2 ULg)
Full Text
Peer Reviewed
See detailNew analogues of the KATP channel opener cromakalim : synthesis and pharmacological evaluation on rat pancreatic B-cells and rat aorta rings
Sebille, S.; De Tullio, Pascal ULg; Antoine, M. H. et al

in Fundamental & Clinical Pharmacology (2004)

Detailed reference viewed: 32 (4 ULg)
Full Text
Peer Reviewed
See detailNew trends in the development of positive allosteric modulators of AMPA receptors
Graindorge, E.; Francotte, Pierre ULg; Boverie, S. et al

in Current Medicinal Chemistry - Central Nervous System Agents (2004), 4

Detailed reference viewed: 2 (0 ULg)
Full Text
Peer Reviewed
See detailProgress in the field of GPIIb/IIIa antagonists
Hanson, Julien ULg; De Leval, X.; David, Jean-Louis ULg et al

in Current Medicinal Chemistry - Cardiovascular and Hematological Agents (2004), 2

Detailed reference viewed: 15 (1 ULg)
Full Text
Peer Reviewed
See detailEffects of cromakalim analogues on rat pancreatic B-cells, rat aorta rings and rat uterus. Study of their mechanism of action as potassium channel activators
Sebille, S.; Boverie, S.; Becker, B. et al

in Fundamental & Clinical Pharmacology (2004)

Detailed reference viewed: 13 (1 ULg)
Full Text
Peer Reviewed
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

Detailed reference viewed: 11 (2 ULg)
Full Text
Peer Reviewed
See detailIdentification of COX-2 selective inhibitor
Michaux, C.; Julémont, F.; de Leval, X. et al

in Fundamental & Clinical Pharmacology (2004)

Detailed reference viewed: 6 (1 ULg)
Full Text
Peer Reviewed
See detailPharmacological characterization of N-tert-butyl-N’-[2-(4’-methylphenylamino)-5-nitrobenzenesulfonyl]urea (BM-573), a novel thromboxane A2 receptor antagonist and thromboxane synthase inhibitor in a rat model of arterial thrombosis and its effects on bleeding time
Dogné, Jean-Michel ULg; Hanson, Julien ULg; De leval, X. et al

in Journal of Pharmacology and Experimental Therapeutics (The) (2004), 309(2), 498-505

The present study was undertaken to characterize the antiplatelet and antithrombotic effects of BM-573 [N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl] urea], an original combined ... [more ▼]

The present study was undertaken to characterize the antiplatelet and antithrombotic effects of BM-573 [N-tert-butyl-N'-[2-(4'-methylphenylamino)-5-nitrobenzenesulfonyl] urea], an original combined thromboxane receptor antagonist and thromboxane synthase inhibitor in rats, and to determine its effects on mice bleeding time. Intraperitoneal injection of a single dose of 5 mg/kg BM-573 to rats inhibited U-46619 (9,11-dideoxy-9,11-methanoepoxy-prostaglandin F-2)-induced washed platelet aggregation 30 min and 1, 2, and 4 h after drug administration with a maximum antiplatelet effect observed after 1 and 2 h. In a rat model of thrombosis induced by ferric chloride application on the abdominal aorta, BM-573 significantly reduced the thrombus weight by 92.53, 80.20, 64.75, and 18.21% at doses of 5, 2, 0.5, and 0.2 mg/kg, respectively. Time to occlusion of abdominal aorta in the BM-573-treated group (41.50+/-5.21 min) was significantly prolonged compared with the vehicle-treated rats (16.16+/-0.79 min). Like furegrelate, seratrodast, and acetylsalicylic acid, BM-573 did not affect the tail bleeding time induced by tail transection in mice compared with vehicle-treated mice. Moreover, BM-573, a close derivative of the loop diuretic torasemide, failed to induce a significant increase in diuresis in rat and did not produce a decrease in blood glucose concentration as observed with the sulfonylurea glibenclamide. In conclusion, we have demonstrated that the nitrobenzenic sulfonylurea BM-573, an original combined thromboxane receptor antagonist and thromboxane synthase inhibitor, is a potent antithrombotic agent that does not affect bleeding time. Moreover, BM-573 lost the diuretic property of torasemide and has no impact on glycemia. [less ▲]

Detailed reference viewed: 55 (16 ULg)
Full Text
Peer Reviewed
See detailRecent development in the field of dual COX / 5-LOX inhibitors
Julémont, F.; Dogné, J.-M.; Pirotte, Bernard ULg et al

in Mini Reviews in Medicinal Chemistry (2004), 4

Detailed reference viewed: 7 (1 ULg)
Full Text
Peer Reviewed
See detailDesign and pharmacological evaluation of recently developed 6-substituted 3-bromophenyl 2-oxo-2H-1-benzopyran 3-carboxylate derivatives as putative inhibitors of cell invasion
Kempen, I.; Frankenne, F.; Telliez, A. et al

in Fundamental & Clinical Pharmacology (2004)

Detailed reference viewed: 5 (0 ULg)