Crystal structure of 7-chloro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide, C10H12CIN3O2S

in Zeitschrift für Kristallographie. New Crystal Structures (2005), NCS 220

4,6-Disubstitued 2,2-dimethylchromans structually related to the KATP channel opener cromakalim : design, synthesis, and effect on insulin release and vascular tone

in Journal of Medicinal Chemistry (2005), 48

Effect on KATP channel activation properties and tissue selctivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine

in Journal of Medicinal Chemistry (2005), 48

3,6-Disubstitued coumarins as mechanism-based inhibitors of thrombin and factor Xa

in Journal of Medicinal Chemistry (2005), 48

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 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 ▲]

Novel thiadiazine derivatives useful as AMPA receptor modulators, preparation method, and pharmaceutical compositions containing them

Patent (2004)

Improvement of the pharmacophoric model for an agonistic activity of arylthiadiazine dioxides on pancreatic KATP channels using the CoMSIA approach

Poster (2004, August)

Modulation of the arachidonic cascade with omega 3 fatty acids or analogues: Potential therapeutic benefits

in Mini-Reviews in Medicinal Chemistry (2004), 4(6), 659-668

Increasing interest in the role of omega 3 fatty acids has arisen in these latest years since evidence of their implication in the cardioprotective fish based diet of the Inuit has been demonstrated ... [more ▼]

Increasing interest in the role of omega 3 fatty acids has arisen in these latest years since evidence of their implication in the cardioprotective fish based diet of the Inuit has been demonstrated. Furthermore, several in vitro, in vivo and epidemiological studies support the benefit of this fatty acids intake in various pathological states such as in the cardiovascular, cancer, inflammation, psychiatric, paediatric, pulmonary, dermatological and ophthalmologic fields. This review will focus on metabolism and pharmacological implication of w3 fatty acids intake as well as its interest in the prevention or treatment of the above-mentioned pathologies. [less ▲]

Relaxant effects on the rat uterine smooth muscle of putative K+ATP channel openers

Poster (2004, July)

Identification d’inhibiteurs sélectifs de la cyclooxygénase-2 (COX-2)

Conference (2004, June)