A5020092970- Fibroblast Growth Factor Research
- Blood Coagulation and Thrombosis Mechanisms
- Oxidative Organic Chemistry Reactions
- Atrial Fibrillation Management and Outcomes
- Heparin-Induced Thrombocytopenia and Thrombosis
- Synthetic Organic Chemistry Methods
- Kruppel-like factors research
- Organometallic Complex Synthesis and Catalysis
- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- Antiplatelet Therapy and Cardiovascular Diseases
- Epigenetics and DNA Methylation
- Cancer Treatment and Pharmacology
- Advanced Synthetic Organic Chemistry
- Proteoglycans and glycosaminoglycans research
- Click Chemistry and Applications
- Inorganic and Organometallic Chemistry
- Asymmetric Synthesis and Catalysis
- Synthesis and Reactivity of Heterocycles
- Synthesis of heterocyclic compounds
- Synthesis of β-Lactam Compounds
- Chemical synthesis and pharmacological studies
- Molecular spectroscopy and chirality
- Chemical Synthesis and Reactions
- Synthesis and Biological Evaluation
- Helicobacter pylori-related gastroenterology studies
Sanofi (France)
2002-2014
The Ohio State University
1993-2003
Centre National de la Recherche Scientifique
1989-1990
Université de Rennes
1989-1990
Laboratoire de Chimie Organique
1990
École Nationale Supérieure de Chimie de Rennes
1990
Despite the importance of microbiota in human physiology, molecular bases that govern interactions between these commensal bacteria and their host remain poorly understood. We recently reported sulfatases play a key role adaptation major bacterium, Bacteroides thetaiotaomicron, to its (Benjdia, A., Martens, E. C., Gordon, J. I., Berteau, O. (2011) Biol. Chem. 286, 25973-25982). hypothesized are instrumental for this related species, metabolize highly sulfated glycans (i.e. mucins...
In the search of a potential backup for clopidogrel, we have initiated HTS campaign designed to identify novel reversible P2Y12 antagonists. Starting from hit with low micromolar binding activity, report here main steps optimization process leading identification preclinical candidate SAR216471. It is potent, highly selective, and receptor antagonist by far most potent inhibitor ADP-induced platelet aggregation among antagonists described in literature. SAR216471 displays vivo antiplatelet...
Fibroblast growth factor (FGF) signaling regulates mammalian development and metabolism, its dysregulation is implicated in many inherited acquired diseases, including cancer. Heparan sulfate glycosaminoglycans (HSGAGs) are essential for FGF as they promote FGF.FGF receptor (FGFR) binding dimerization. Using novel organic synthesis protocols to prepare homogeneously sulfated heparin mimetics (HM), hexasaccharide (HM(6)), octasaccharide (HM(8)), decasaccharide (HM(10)), we tested the ability...
Compound 15 (SAR107375), a novel potent dual thrombin and factor Xa inhibitor resulted from rational optimization process. Starting compound 14, with low modest anti-thrombin inhibitory activities (IC50's of 3.5 0.39 μM, respectively), both were considerably improved, notably through the incorporation neutral chlorothiophene P1 fragment tuning P2 P3-P4 fragments. Final metabolic stability microsomes led to identification 15, which displays strong activity in vitro vs (with Ki's 1 8 nM,...
SSR182289A competitively inhibits human thrombin (K(i) = 0.031 +/- 0.002 microM) and shows good selectivity with respect to other proteases, e.g., trypsin 54 2 microM), factor Xa 167 9 VIIa, IXa, plasmin, urokinase, tPA, kallikrein, activated protein C (all K(i) values >250 microM). In plasma, demonstrated anticoagulant activity in vitro as measured by standard clotting parameters (EC100 time 96 7 nM) inhibited tissue factor-induced generation (IC50 of 0.15 0.02 thrombin-induced aggregation...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStudies directed toward the total synthesis of cerorubenic acid-III. 2. Analysis inability to realize D ring formation by means extraannular Robinson annulationLeo A. Paquette, Gilbert Y. Lassalle, and Carl J. LovelyCite this: Org. Chem. 1993, 58, 16, 4254–4261Publication Date (Print):July 1, 1993Publication History Published online1 May 2002Published inissue 1 July...
Abstract The easy transformation of pyrrolidine 4 in 5 and then into 7 shows that the diethylacetal 3‐cyano 2‐propenal can be considered as a useful synthetic equivalent functionnalized heterocumulenes 2 3.
Abstract The 1,2,5‐triphenyl‐3,4‐cis‐divinylpyrrolidine (I) reacts with iron pentacarbonyl (II) to give the triphenyldiethylpyrrole (III) and vinylpyrroline (IV).
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at glance that was extracted from about 100 leading journals. To access of an article which published elsewhere, please select “Full Text” option. The original trackable via the “References”