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Artigo Revisado por pares

M Speich, Claire M eacute tayer, P Arnaud, Van Goc Nguyen, Henri-Louis Boiteau,

Four groups of 6 rabbits were subjected to the following diets for 25 weeks: I (controls), II (water with 9.66 µmol/l of lead), III (atherogenic) and IV (atherogenic + 9.66 µmol/l of lead). Lead, magnesium, calcium, zinc and cadmium were then analyzed in 20 dry tissues. At the level of the arteries, veins and skin a tendency was observed toward increased lead concentration in rabbits of groups II and IV, elevated calcium levels in groups III and IV (a tenfold increase of calcium in the aortas), and a higher ...

Tópico(s): Heavy Metal Exposure and Toxicity

1983 - Karger Publishers | Annals of Nutrition and Metabolism

Artigo Revisado por pares

Jean‐Guy Boiteau, Gilles Ouvry, Jean-Marie Arlabosse, Stéphanie Astri, Audrey Beillard, Yushma Bhurruth-Alcor, Laetitia Bonnary, Claire Bouix‐Peter, Karine Bouquet, Marilyne Bourotte, Isabelle Cardinaud, Catherine Comino, Benoît Déprez, Denis Duvert, A. Feret, Fériel Hacini‐Rachinel, Craig S. Harris, Anne‐Pascale Luzy, Arnaud Mathieu, Corinne Millois, Nicolas Orsini, Jonathan Pascau, Artur Pinto, David Piwnica, Gaëlle Polge, Arnaud Reitz, Kevin Reversé, Nicolas Rodeville, Patricia Rossio, Delphine Spiesse, Samuel Tabet, Nathalie Taquet, Loïc Tomas, Emmanuel Vial, Laurent Hennequin,

Targeting the TNFα pathway is a validated approach to the treatment of psoriasis. In this pathway, TACE stands out as a druggable target and has been the focus of in-house research programs. In this article, we present the discovery of clinical candidate 26a. Starting from hits plagued with poor solubility or genotoxicity, 26a was identified through thorough multiparameter optimisation. Showing robust in vivo activity in an oxazolone-mediated inflammation model, the compound was selected for development. ...

Tópico(s): Synthesis and biological activity

2017 - Elsevier BV | Bioorganic & Medicinal Chemistry

Artigo Revisado por pares

Samuel Tabet, Nicolas Rodeville, Arnaud Mathieu, Catherine Raffin, Corinne Millois-Barbuis, Branislav Musicki, Franck Muller, Thibaud Gerfaud, Jean‐Guy Boiteau, Isabelle Cardinaud,

Efforts toward a convenient and scalable process for the synthesis of a novel CXCR antagonist 1 are described, with a specific focus on a chiral key intermediate. Two generations of a racemic route have been developed for short-term deliveries, and a stereoselective process has been devised for longer term plans. Key steps involved an enzymatic resolution of racemic tetrahydrothiophene-2-carboxylic acid to install the (2R) stereocenter, the mild and efficient preparation of a sterically hindered ...

Tópico(s): Click Chemistry and Applications

2017 - American Chemical Society | Organic Process Research & Development

Artigo Revisado por pares

M Speich, Claire M eacute tayer, P Arnaud, Van Goc Nguyen, Bernard Bousquet, Henri-Louis Boiteau,

Changes in concentrations of blood lead, cholesterol, tnacylglycerols, GOT and GPT enzymes, phosphorus, proteins, plasma calcium and magnesium, and erythrocyte magnesium were studied for 25 weeks in 4 groups of 6 rabbits each receiving different diets: I (controls), II (water with 9.66 µmol/l of lead), III (atherogenic) and IV (atherogenic + 9.66 µmol/l of lead). Differences observed, with respect to the diets, for lead, cholesterol, enzymes, proteins and erythrocyte magnesium were evident from the 42nd ...

Tópico(s): Effects and risks of endocrine disrupting chemicals

1983 - Karger Publishers | Annals of Nutrition and Metabolism