Identification d’un inhibiteur COX-2 sélectif », 18èmes Journées Franco-belges de Pharmacochimie

Poster (2004, June)

Synthèse et évaluation pharmacologique de nouveaux antagonistes du récepteur au thromboxane A2 dérivés du BM-573

Poster (2004, June)

Synthèse de nouveaux analogues benzothiadiaziniques en tant qu’activateurs potentiels des canaux KATP et leur évaluation pharmacologique in vitro sur cellules B pancréatiques, aorte et utérus de rats

Poster (2004, June)

In vivo evaluation of antithrombotic potency of BM-613, a thromboxane A2 receptor antagonist, in a rat model of arterial thrombosis

Conference (2004, May)

Development of thromboxane A2 modulators as promising anti-metastatic and anti-angiogenic compounds

Conference (2004, May)

Effects of COX-2 inhibitors on ROS produced by Chlamydia pneumoniae-primed human promonocytic cells (THP-1)

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 lM) 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. [less ▲]

Recent developments in the chemistry of potassium channel activators : the cromakalim analogues

in Current Medicinal Chemistry (2004), 11

Modulation of the arachidonic cascade with omega3 fatty acids or analogues: potential therapeutic benefits

in Mini Reviews in Medicinal Chemistry (2004), 4

Effects of COX-2 inhibitors on ROS produced by Chlamydia pneumoniae-primed human promonocytic cells (THP-1)

in Biochemical and Biophysical Research Communications (2004), 325

New trends in the development of positive allosteric modulators of AMPA receptors

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