Design, Synthesis and Pharmacological Evaluation of R/S-3,4-Dihydro-2,2-Dimethyl-6-Halo-4-(Phenylaminocarbonylamino)-2H-1-Benzopyrans: Towards Tissue-Selective Pancreatic Beta-Cells KATP Channel Openers Structually Related to (+/-)-Cromakalim

in Journal of Medicinal Chemistry (2006), 49

Three-Dimentional Quantitative Structure-Activity Relationships of ATP-Sensitive Potassium (KATP) Channel Openers Belonging to the 3-Alkylamino-4H-1,2,4-benzo- and 3-Alkylamino-4H-1,2,4-pyridothiadiazine 1,1-Dioxide Families

in Journal of Medicinal Chemistry (2006), 49

Benzopyran derivatives, method of production and use thereof

Patent (2005)

Preparation of fluorinated benzothiadiazine derivatives and their use as AMPA receptor modulators

Patent (2005)

Vers la découverte d’activateurs sélectifs du canal KATP pancréatique, analogues du cromakalim : synthèse et évaluation pharmacologique du R/S-4-(4-chlorophénylaminothiocarbonylamino)-3,4-dihydro-2,2-diméthyl-6-fluoro-2H-1-benzopyrane

Poster (2005, May)

Synthesis and pharmacological effects of opened analogues of benzothiadiazine 1,1-dioxides with sulfonylurea moieties on diuresis and glycemia

Poster (2005, May)

Synthèse et évaluation biologique d’analogues 6,7-disubstitués du (R)-3-[2-(1-hydroxypropylamino)]-4H-1,2,4-benzothiadiazine 1,1-dioxyde en tant qu’activateurs potentiels des canaux potassiques sensibles à l’ATP et leurs analogues biotinylés en tant qu’outils pharmacologiques

Poster (2005, May)

Développement de modulateurs de la voie du thromboxane A2 en tant qu’agents anti-angiogéniques et anti-métastatiques

Poster (2005, May)

Characterization of an original model of myocardial infarction provoked by coronary artery thrombosis induced by ferric chloride in pig

in Thrombosis Research (2005), 116(5), 431-442

Background: Great advances have been made in the prevention of thrombotic disorders by developments of new pharmacological and surgical treatments. Animal models of arterial thrombosis have largely ... [more ▼]

Background: Great advances have been made in the prevention of thrombotic disorders by developments of new pharmacological and surgical treatments. Animal models of arterial thrombosis have largely contributed to the discovery and to the validation of original treatments. The purpose of the present work was to develop and validate an original model of acute myocardial infarction provoked in pig by thrombosis of the left anterior descending (LAD) coronary artery induced by topical application of ferric chloride solution. Methods and results: Myocardial infarction, resulting from an occlusive and adherent mixed thrombus formed in the LAD coronary artery, was examined at macroscopic level using dual staining technique (Evans blue dye; triphenyltetrazolium chloride) and at microscopic level using conventional histological analyses and immunohistochemical detection of desmin. Biochemical markers (troponin T and ATP), platelet reactivity and standard hemodynamic parameters (such as stroke volume, ejection fraction, stroke work and cardiac output) have also been evaluated. From these analyses, it was demonstrated that each pig developed a transmural area of irreversible damage mainly located in the anteroseptal region of the left ventricle. The more progressive development of coronary artery occlusion, as compared to an abrupt Ligation, was accompanied by a correspondingly progressive impairment in hemodynamics. Conclusion: We conclude that this original porcine model of myocardial infarction is quite close to clinical pathophysiological conditions, such as thrombus formation occurring after atherosclerotic plaque rupture. This certainly constitutes a further argument in favour of this model to assess pharmaceutical or mechanical support of an acutely ischemic heart. (c) 2005 Elsevier Ltd. All rights reserved. [less ▲]

Crystal structure of 7-chloro-3-isopropylsulfanyl-4H-1,2,4-benzothiadiazine 1,1-dioxide, C10H11CIN2O2S2

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