Zobrazeno 1 - 10
of 61
pro vyhledávání: '"Nathalie Chauret"'
Autor:
Simon Giroux, Nigel Ewing, Youssef L. Bennani, Francoise Berlioz-Seux, Rebecca S. Shawgo, Anne-Laure Grillot, Nathalie Chauret, Kevin M. Cottrell, Laval C. Chan, Evelyne Dietrich, Francois Denis, Morris Mark A, John Maxwell, Sanjoy Kumar Das, Lucille L’Heureux, Darius Bilimoria, T. Jagadeeswar Reddy, Subajini Selliah, Caroline Cadilhac, Olivier Nicolas, Jinwang Xu, James A. Henderson, Nagraj Mani
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:936-939
The discovery of C2-symmetric bis-thienoimidazoles HCV NS5A inhibitors is herein reported. Two straightforward approaches to access the requisite diyne and biphenyl linker moieties are described. This study revealed the paramount importance of the ar
Autor:
Brian S. Luisi, Philip N. Collier, Pan Li, Lauffer David J, Qing Tang, Carl Poisson, Waal Nathan D, Ganesh Iyer, John J. Court, Sanjoy Kumar Das, Olivier Nicolas, B. Govinda Rao, Rebecca S. Shawgo, Laval C. Chan, Steven M. Ronkin, Nathalie Chauret, Suganthi Nanthakumar, Lucille L’Heureux, Darius Bilimoria, Nagraj Mani, Subajini Selliah, Francois Denis, Kishan Chandupatla, Constantin Yannopoulos, Warren Dorsch, Jeremy Green, Andrzej Ardzinski
Publikováno v:
Journal of medicinal chemistry. 59(13)
The hepatitis C viral proteins NS3/4A protease, NS5B polymerase, and NS5A are clinically validated targets for direct-acting antiviral therapies. The NS5B polymerase may be inhibited directly through the action of nucleosides or nucleotide analogues
Autor:
W. Cameron Black, Jean-François Lévesque, Denis Riendeau, Jean-Pierre Falgueyret, Kevin P. Bateman, M. David Percival, Elise Isabel, Tammy LeRiche, Vouy Linh Truong, Jacques Yves Gauthier, Michel Therien, Robert Zamboni, Sevgi B. Rodan, Sylvie Desmarais, Christophe Mellon, Deborah A. Nicoll-Griffith, Renata Oballa, Gregg Wesolowski, Sonia Lamontagne, Carmai Seto, Nathalie Chauret, Chun Sing Li, Robert N. Young, Frédéric Massé, Wanda Cromlish, Daniel J. McKay, Le T. Duong, Cheuk K. Lau, Serge Leger, Joel Robichaud, Gideon A. Rodan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:887-892
MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat K. It is orally bioavailable and exhibits long half-life in pre-clinical species. In vivo st
Autor:
Olivier Nicolas, Samuel S. Lee, Maribel Rodriguez-Torres, Curtis Cooper, Eric Lawitz, Jean Bedard, Frank H. Anderson, Peter Ghali, Nathalie Chauret, L. Proulx, Isabel Boivin, Roch Thibert
Publikováno v:
Journal of Hepatology. 51:39-46
Background/Aims VCH-759 is a non-nucleoside inhibitor of HCV RNA-dependent polymerase with sub-micromolar IC 50 values versus genotype 1a/1b replicons. Methods The antiviral activity, pharmacokinetics and tolerability of VCH-759 administered as monot
Autor:
Christopher I. Bayly, Jean-François Truchon, Carl Berthelette, Renata Oballa, Stephen Day, Sheldon Crane, Nathalie Chauret
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:998-1002
Nitrile-based inhibitors of cathepsin K have been known for some time and mechanism-of-action studies have demonstrated that cysteinyl proteases interact with nitriles in a reversible fashion. Three main classes of nitrile-containing inhibitors have
Autor:
Jean François Lévesque, Matt Braun, Robert Zamboni, Claudio Sturino, Laird A. Trimble, Robert N. Young, Deborah A. Nicoll-Griffith, Stephen Day, Carmai Seto, Nathalie Chauret, Carl Berthelette, Yves Aubin, Jean-François Truchon, José M. Silva, Nicolas Lachance, Zhaoyin Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:301-304
Metabolites of the potent DP antagonist, MK-0524, were generated using in vitro systems including hepatic microsomes and hepatocytes. Four metabolites (two hydroxylated diastereomers, a ketone and an acyl glucuronide) were characterized by LC-MS/MS a
Autor:
Vincent Pichette, François A. Leblond, Line Ste-Marie, Marie-Claude Duquet, Chantal Boudreau, Marc-Olivier Boily, Nathalie Chauret, Julie Laterreur, Jean-François Lévesque
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 43(12)
1-Aminobenzotriazole (ABT) is regularly used in vivo as a nonspecific and irreversible cytochrome P450 inhibitor to elucidate the role of metabolism on the pharmacokinetic profile of xenobiotics. However, few reports have considered the recent findin
Autor:
Yves Girard, Dwight Macdonald, Deborah A. Nicoll-Griffith, Michel Gallant, Nathalie Chauret, Daniel Dube, Anthony Mastracchio, Laird A. Trimble, Kevin P. Bateman, José M. Silva, Stephen Day, Helene Perrier
Publikováno v:
Journal of Mass Spectrometry. 41:771-780
L-454,560 is a potent phospodiesterase 4 (PDE4) inhibitor which was identified as a development candidate for the treatment of asthma and chronic obstructive pulmonary disease (COPD). As part of the discovery of this compound, interspecies in vitro m
Autor:
Dwight Macdonald, Anthony Mastracchio, Hélène Perrier, Daniel Dubé, Michel Gallant, Patrick Lacombe, Denis Deschênes, Bruno Roy, John Scheigetz, Kevin Bateman, Chun Li, Laird A. Trimble, Stephen Day, Nathalie Chauret, Deborah A. Nicoll-Griffith, Jose M. Silva, Zheng Huang, France Laliberté, Susana Liu, Diane Ethier, Doug Pon, Eric Muise, Louise Boulet, Chi Chung Chan, Angela Styhler, Stella Charleson, Joseph Mancini, Paul Masson, David Claveau, Donald Nicholson, Mervyn Turner, Robert N. Young, Yves Girard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5241-5246
The discovery and SAR of a new series of substituted 8-arylquinoline PDE4 inhibitors are herein described. This work has led to the identification of several compounds with excellent in vitro and in vivo profiles, including a good therapeutic window
Publikováno v:
Rapid Communications in Mass Spectrometry. 19:1984-1992
Discovery stage studies that address issues of absorption, distribution, metabolism and excretion (ADME) are vital for lead optimization resulting in new drug candidates. Often pharmacokinetics (PK) is assessed in these experiments without regard for