641 research outputs found
[4-(2H-1,2,3-benzotriazol-2-yl)phenoxy]alkanoic acids as agonists of peroxisome proliferator-activated receptors (PPARs)
No full textA series of [4-(2H-1,2,3-benzotriazol-2-yl)phenoxy]alkanoic acids has been synthesized and tested as agonists of Peroxisome Proliferator-Activated Receptor (PPAR) a, g, and d. Three compds. displayed 56 to 96% of maximal activity of the ref. drug Wy-14643 on PPARa, and two of these, i.e., 1 and 5, exhibited also moderate activity on either PPARg or d with efficacy equal to 50% and 46% of that of rosiglitazone and GW 501516, resp. Thus, compds. 1 and 5 represent interesting starting point for prepg. novel agents for the treatment of dyslipidemia or of dyslipidemic type-2 diabetes
PROGRESS IN THE TOTAL SYNTHESIS OF SPIROLIDE C AND A MODEL SYSTEM OF A KEY DIELS-ALDER MACROCYCLIZATION
No full textSpirolode C is a macrocyclic marine toxin produced by the dinoflagellate Alexandrium ostenfeldii that has attracted significant synthetic interest due in particular to its rare spirocyclic imine fragment. The work presented herein details progress made in the synthesis of a model system that will be used to optimize reaction conditions for a biomimetic macrocycle closing Diels-Alder reaction in our planned total synthesis. The synthesis of the model system required an extension of our isomerization/Claisen rearrangement (ICR) to be compatible with new vinyl bromide-containing substrates. New conditions to affect the ICR of these challenging substrates were successfully developed, and this led to significant progress in the synthesis of the desired model system
1.1. Le cadre environnemental et son évolution à l'échelle microrégionale
No full textBarral (Coord.), Billoin (D.), Blin (S.), Bossuet (G.), Cramatte (C.), Fruchart (C.) Laplaige (C.), Mamie (A.), Monnier (J.), Mougin (P.), Nouvel (P.), Piningre (J.-F.), Thivet (M.), Nouvelles données sur l’agglomération antique d’Epomanduodurum (Mandeure et Mathay, Doubs)International audienc
Residual macrovascular risk in 2013: What have we learned?
No full textCardiovascular disease poses a major challenge for the 21st century, exacerbated by the pandemics of obesity, metabolic syndrome and type 2 diabetes. While best standards of care, including high-dose statins, can ameliorate the risk of vascular complications, patients remain at high risk of cardiovascular events. The Residual Risk Reduction Initiative (R3i) has previously highlighted atherogenic dyslipidaemia, defined as the imbalance between proatherogenic triglyceride-rich apolipoprotein B-containing-lipoproteins and antiatherogenic apolipoprotein A-I-lipoproteins (as in high-density lipoprotein, HDL), as an important modifiable contributor to lipid-related residual cardiovascular risk, especially in insulin-resistant conditions. As part of its mission to improve awareness and clinical management of atherogenic dyslipidaemia, the R3i has identified three key priorities for action: i) to improve recognition of atherogenic dyslipidaemia in patients at high cardiometabolic risk with or without diabetes; ii) to improve implementation and adherence to guideline-based therapies; and iii) to improve therapeutic strategies for managing atherogenic dyslipidaemia. The R3i believes that monitoring of non-HDL cholesterol provides a simple, practical tool for treatment decisions regarding the management of lipid-related residual cardiovascular risk. Addition of a fibrate, niacin (North and South America), omega-3 fatty acids or ezetimibe are all options for combination with a statin to further reduce non-HDL cholesterol, although lacking in hard evidence for cardiovascular outcome benefits. Several emerging treatments may offer promise. These include the next generation peroxisome proliferator-activated receptorα agonists, cholesteryl ester transfer protein inhibitors and monoclonal antibody therapy targeting proprotein convertase subtilisin/kexin type 9. However, long-term outcomes and safety data are clearly needed. In conclusion, the R3i believes that ongoing trials with these novel treatments may help to define the optimal management of atherogenic dyslipidaemia to reduce the clinical and socioeconomic burden of residual cardiovascular risk. © 2014 Fruchart et al.; licensee BioMed Central Ltd
1.4. Dynamique du peuplement et formes de l’habitat dans le secteur de Mandeure, entre la fin de l’âge du Fer et le début du Moyen-Âge
No full textBarral (Coord.), Billoin (D.), Blin (S.), Bossuet (G.), Cramatte (C.), Fruchart (C.) Laplaige (C.), Mamie (A.), Monnier (J.), Mougin (P.), Nouvel (P.), Piningre (J.-F.), Thivet (M.), Nouvelles données sur l’agglomération antique d’Epomanduodurum (Mandeure et Mathay, Doubs)International audienc
2.2.2. La trame viaire de l'agglomération Antique et son intégration aux axes de communication
No full textBarral (Coord.), Billoin (D.), Blin (S.), Bossuet (G.), Cramatte (C.), Fruchart (C.) Laplaige (C.), Mamie (A.), Monnier (J.), Mougin (P.), Nouvel (P.), Piningre (J.-F.), Thivet (M.), Nouvelles données sur l’agglomération antique d’Epomanduodurum (Mandeure et Mathay, Doubs)International audienc
2.2.1. L’occupation de l’agglomération antique de Mandeure / Mathay : phases de développement du tissu urbain
No full textBarral (Coord.), Billoin (D.), Blin (S.), Bossuet (G.), Cramatte (C.), Fruchart (C.) Laplaige (C.), Mamie (A.), Monnier (J.), Mougin (P.), Nouvel (P.), Piningre (J.-F.), Thivet (M.), Nouvelles données sur l’agglomération antique d’Epomanduodurum (Mandeure et Mathay, Doubs)International audienc
3.2.1. Le sanctuaire des « Champs des Fougères »
No full textBarral (Coord.), Billoin (D.), Blin (S.), Bossuet (G.), Cramatte (C.), Fruchart (C.) Laplaige (C.), Mamie (A.), Monnier (J.), Mougin (P.), Nouvel (P.), Piningre (J.-F.), Thivet (M.), Nouvelles données sur l’agglomération antique d’Epomanduodurum (Mandeure et Mathay, Doubs)International audienc
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