Zobrazeno 1 - 10
of 69
pro vyhledávání: '"Jacques Yves Gauthier"'
Autor:
Joel Robichaud, Nicolas Morin, Sébastien Gagné, Michel Belley, Lianhai Li, Genevieve Lavallee, Geoffrey K. Tranmer, Yves Gareau, Erin F. Mulrooney, W. Cameron Black, Stacia Kargman, Jean-François Lévesque, Joseph A. Mancini, Jacques Yves Gauthier, Jean-François Fournier, Denis Deschenes, Jin Wu, Martine Hamel, Zhaoyin Wang, Michel Therien, Martin Henault, Yaël Mamane, Huda Hyjazie
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2836-2839
A weak, UDP-competitive antagonist of the pyrimidinergic receptor P2RY(14) with a naphthoic acid core was identified through high-throughput screening. Optimization provided compounds with improved potency but poor pharmacokinetics. Acylglucuronidati
Autor:
Paul Ambrose Lythgo, M. David Percival, Jacques Yves Gauthier, Andriy O. Samokhin, Dieter Brömme
Publikováno v:
Journal of Cardiovascular Pharmacology. 56:98-105
Recent studies provided evidence for a significant role of cathepsin S during extracellular remodeling in atherosclerosis. In this study, we investigated the effect of a specific cathepsin S inhibitor on atherosclerotic plaque progression in the brac
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:
Wanda Cromlish, Vouy-Linh Truong, Chun Sing Li, Jean-François Truchon, Robert Houle, Sylvie Desmarais, Joel Robichaud, W. Cameron Black, Qingping Wang, Isabelle Courchesne, Daniel J. McKay, Frédéric Massé, Marc Ouellet, M. David Percival, Sonia Lamontagne, Jacques Yves Gauthier
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4929-4933
Highly potent, selective, and bioavailable inhibitors of human, mouse, or rat cathepsin S are described. The key structural features combine a sulfonyl moiety attached to a large group in P2 and a small substituent in P3.
Autor:
Serge Leger, Denis Deschenes, Chun Sing Li, Donald B. Kimmel, M. David Percival, Michel Therien, Mary E. McGrath, Robert Zamboni, Daniel J. McKay, Sevgi B. Rodan, Gregg Wesolowski, Denis Riendeau, W. Cameron Black, Jean-Pierre Falgueyret, Sylvie Desmarais, Frédéric Massé, Jacques Yves Gauthier, Vouy-Linh Truong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1985-1989
Based on our previous study with trifluoroethylamine as a P2–P3 amide isostere of cathepsin K inhibitor, further optimization led to identification of compound 22 (L-873724) as a potent and selective non-basic cathepsin K inhibitor. This compound s
Autor:
Sébastien Gagné, Joseph A. Mancini, W. Cameron Black, Jean-François Lévesque, Martine Hamel, Yongxin Han, Jin Wu, Erin F. Mulrooney, Jacques Yves Gauthier, Joel Robichaud, Martin Henault, Stacia Kargman, Nicolas Morin, Yaël Mamane, Jean-François Fournier
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4366-4368
Our series of competitive antagonists against the G-protein coupled receptor P2Y(14) were found to be highly shifted in the presence of serum (>99% protein bound). A binding assay using 2% human serum albumin (HSA) was developed to guide further SAR
Autor:
Jacques Yves Gauthier, Robert Zamboni, José M. Silva, Chun Li, Deborah A. Nicoll-Griffith, Denis Riendeau, Chi-Chung Chan, Patrick Roy, Christine Brideau, Erich L. Grimm, Nathalie Chauret, Michel Therien, Serge Leger, Peppi Prasit, Laird A. Trimble, Robert N. Young, James A. Yergey, Joseph A. Mancini, Zhaoyin Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2683-2686
Metabolites of the COX-2 inhibitor rofecoxib (MK-0966, Vioxx) were prepared by synthetic or biosynthetic methods. Metabolites include products of oxidation, glucuronidation, reduction and hydrolytic ring opening. Based on an in vitro whole blood assa
Autor:
Denis Riendeau, Stella Charleson, Jocelyne Guay, Elizabeth Wong, Denise M. Visco, Robert Gordon, Lijing Xu, Michel Therien, Gillian Greig, Petpiboon Prasit, Chi-Chung Chan, W. Cameron Black, Jacques Yves Gauthier, David Claveau, Erich L. Grimm, Wanda Cromlish, Christine Brideau, Cheuk K. Lau, Chun-Sing Li
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:3181-3186
By inserting an oxygen link between the 3-fluorophenyl and the lactone ring of 5,5-dimethyl-3-(3fluorophenyl)-4-(4-methanesulfonylphenyl)-2 (5H)-furanone 1 (DFU), analogs with enhanced in vitro COX-2 inhibitory potency as well as in vivo potency in m
Autor:
Li Jing Xu, Denise M. Visco, Diane Ethier, Gillian Greig, Denis Riendeau, Jacques Yves Gauthier, Stella Charleson, Chi-Chung Chan, Robert Gordon, Denis Deschenes, Yves Girard, Richard Friesen, Robert N. Young, Elizabeth Wong, Christine Brideau, Chantal Savoie, Daniel Dube, Zhaoyin Wang, Rejean Fortin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:2777-2782
A series of novel 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines has been synthesized and evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-1, and COX-2. Optimum COX-2 activity is observed by introduction of a su
Autor:
C. S. Mcfarlane, Robert Zamboni, C. Rochette, M. McAuliffe, Claude Dufresne, P. Prasit, Jacques-Yves Gauthier, Nicole Sawyer, P. Roy, Kathleen M. Metters, Thomas R. Jones, Daniel Guay
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:453-458
The structure-activity relationship of a series of styrylpyridine analogs of MK-0476 (montelukast, Singulair) is described. This work has led to the identification of a number of potent and orally active cysLT1 receptor (LTD4 receptor) antagonists in