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32 results on '"Brayer, Jean‐Louis"'

20. New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors

Author

Legros, Céline, primary, Matthey, Ulrich, additional, Grelak, Teresa, additional, Pedragona-Moreau, Sandrine, additional, Hassler, Werner, additional, Yous, Saïd, additional, Thomas, Emmanuel, additional, Suzenet, Franck, additional, Folleas, Benoît, additional, Lefoulon, François, additional, Berthelot, Pascal, additional, Caignard, Daniel-Henri, additional, Guillaumet, Gérald, additional, Delagrange, Philippe, additional, Brayer, Jean-Louis, additional, Nosjean, Olivier, additional, and Boutin, Jean, additional

Published
2013
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25. Diastereodivergent Pictet-Spengler Cyclization of Bicyclic N-Acyliminium Ions: Controlling a Quaternary Stereocenter.

Author

de Carné‐Carnavalet, Benoît, Krieger, Jean‐Philippe, Folléas, Benoît, Brayer, Jean‐Louis, Demoute, Jean‐Pierre, Meyer, Christophe, and Cossy, Janine

Subjects
PICTET-Spengler reaction, CONDENSATION reactions, IONS, ELECTRONS, PROTON transfer reactions
Abstract

The diastereoselectivity of the Pictet-Spengler cyclization of bicyclic N-acyliminium ions that contain a 3-azabicyclo[ n.3.0]alkane core and an electron-rich π-nucleophilic moiety, such as an indol-2-yl, indol-3-yl, 1-methylpyrrol-2-yl, or 3,5-dimethoxyphenyl group, was examined. The N-acyliminium ions were generated by protonation of the corresponding enamides or hemiaminals, which were derived from imides. Control of the quaternary stereocenter created at the newly formed ring junction was achieved in a diastereodivergent manner by fine-tuning the reaction conditions, which determined whether the reaction proceeded under kinetic or thermodynamic control. Mechanistic studies indicated that a retro-Pictet-Spengler reaction pathway is involved in the equilibration process. [ABSTRACT FROM AUTHOR]

Published
2015
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29. New Radioligands for Describing the Molecular Pharmacology of MT1 and MT2 Melatonin Receptors.

Author

Legros, Céline, Matthey, Ulrich, Grelak, Teresa, Pedragona-Moreau, Sandrine, Hassler, Werner, Yous, Saïd, Thomas, Emmanuel, Suzenet, Franck, Folleas, Benoît, Lefoulon, François, Berthelot, Pascal, Caignard, Daniel-Henri, Guillaumet, Gérald, Delagrange, Philippe, Brayer, Jean-Louis, Nosjean, Olivier, and Boutin, Jean A.

Subjects
MELATONIN, RADIOLABELING, CIRCADIAN rhythms, PHARMACOLOGY, MOLECULES, MAMMALS
Abstract

Melatonin receptors have been studied for several decades. The low expression of the receptors in tissues led the scientific community to find a substitute for the natural hormone melatonin, the agonist 2-[125I]-iodomelatonin. Using the agonist, several hundreds of studies were conducted, including the discovery of agonists and antagonists for the receptors and minute details about their molecular behavior. Recently, we attempted to expand the panel of radioligands available for studying the melatonin receptors by using the newly discovered compounds SD6, DIV880, and S70254. These compounds were characterized for their affinities to the hMT1 and hMT2 recombinant receptors and their functionality in the classical GTP S system. SD6 is a full agonist, equilibrated between the receptor isoforms, whereas S70254 and DIV880 are only partial MT2 agonists, with Ki in the low nanomolar range while they have no affinity to MT1 receptors. These new tools will hopefully allow for additions to the current body of information on the native localization of the receptor isoforms in tissues. [ABSTRACT FROM AUTHOR]

Published
2013
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32. ChemInform Abstract: Chiral α-Amino Phosphonates via Rhodium-Catalyzed Asymmetric 1,4-Addition Reactions.

Author

Lefevre, Nicolas, Brayer, Jean‐Louis, Folleas, Benoit, and Darses, Sylvain

Subjects
*PHOSPHONATES, *ORGANIC synthesis, *CHIRALITY, *RHODIUM catalysts, *ADDITION reactions, *ASYMMETRY (Chemistry), *BORATES, *LIGANDS (Chemistry)
Abstract

A straightforward method for the synthesis of α-aminophosphonates from dehydroaminophosphonates (I) and (IV) is developed using a Rh-catalyzed 1,4-addition of arenetrifluoroborates in the presence of (S)-difluorophos as chiral ligand. [ABSTRACT FROM AUTHOR]

Published
2014
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