Zobrazeno 1 - 10
of 37
pro vyhledávání: '"Serge Leger"'
Autor:
Dan Tulpan, Serge Leger
Publikováno v:
The Plant Genome, Vol 10, Iss 1 (2017)
Worldwide genome sequencing efforts for plants with medium and large genomes require identification and visualization of orthologous genes, while their syntenic conservation becomes the pinnacle of any comparative and functional genomics study. Using
Externí odkaz:
https://doaj.org/article/d6d29be0cad04fb3a7b6c50617da039e
Autor:
Félix Chagnon, Lee Fader, Dorich Stéphane, Bin Chen, Jason Burch, St-Onge Miguel, Serge Leger, Jennifer H. Cox
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127104
Novel prostaglandin E2 receptor 4 (EP4) agonists featuring a pyridone core and an allylic alcohol ω-chain were discovered. These agonists were shown to be selective over EP1, EP2 and EP3. Analogs harboring a 4-carboxylic acid phenethyl α-chain disp
Autor:
Zheng Huang, Jocelyne Guay, Lei Zhang, David A. Powell, Joel Robichaud, Elise Isabel, Jean-Philippe Leclerc, Cameron Black, Serge Leger, Renata Oballa, Sébastien Guiral, Sheldon Crane, Chun Sing Li, Yeeman K. Ramtohul
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5692-5696
Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for efficacy and to avoid SCD1 inhibition in the skin and eye
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:
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
Publikováno v:
Tetrahedron Letters. 43:1147-1150
The synthesis of the pyran segment of (+)-acutiphycin was achieved using an intramolecular Lewis acid-catalyzed reaction between a silyl enol ether and an ortho ester.
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:
Diane Ethier, Philip Tagari, Richard Frenette, H. Piechuta, C. C. Chan, Denis Riendeau, Michel Therien, M. McAuliffe, Yves Girard, John H. Hutchinson, Christine Brideau, Stella Charleson, Thomas R. Jones, Jocelyne Guay, Serge Leger
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2391-2396
This paper reports on the SAR investigation of inhibitors of 5-lipoxygenase activating protein (FLAP) based on MK-0591. Emphasis was made on modifications to the nature of the link between the indole and the quinoline moieties, to the substitution pa
Autor:
Robert Zamboni, Jocelyne Guay, Stella Charleson, M.D. Percival, Jean-Pierre Falgueyret, Joseph A. Mancini, Susan Boyce, Michael J. Therien, Lijing Xu, R. Gordon, Stacia Kargman, Anthony W. Ford-Hutchinson, Gillian Greig, Marc Ouellet, Denis Riendeau, Petpiboon Prasit, Serge Leger, Zhaoyin Wang, J.K. Webb, Diane Ethier, Chi-Chung Chan, Gary P. O'Neill, Robert N. Young, Ian W. Rodger, Wanda Cromlish, Christine Brideau, Jillian F. Evans, Michael J. Gresser, E. Wong
Publikováno v:
British Journal of Pharmacology. 121:105-117
1. DFU (5,5-dimethyl-3-(3-fluorophenyl)-4-(4-methylsulphonyl)phenyl-2(5H)-furan one) was identified as a novel orally active and highly selective cyclo-oxygenase-2 (COX-2) inhibitor. 2. In CHO cells stably transfected with human COX isozymes, DFU inh
Autor:
Philip J. Vickers, Denis Riendeau, Philip Tagari, W. Cameron Black, Brian P. Kennedey, Cheuk K. Lau, Yves Leblanc, Jacques Yves Gauthier, Jocelyne Guay, Serge Leger, P. Prasit, Diane Ethier, Robert Gordon, Lijing Xu, Zhaoyin Wang, Joseph A. Mancini, Elizabeth Wong, Wanda Cromlish, Chi-Chung Chan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:87-92
The thiophene ring of DuP 697 was replaced by a variety of heterocycles and the products were tested for their ability to inhibit human Cox-2 and Cox-1, the isozymes of cyclooxygenase.