Zobrazeno 1 - 10
of 36
pro vyhledávání: '"Claudio Sturino"'
Autor:
Jun Chen, Baihua Hu, Kevin M. Johnson, Kang-Jye Chou, Jack A. Terrett, Yunli Wang, Lea Constantineau-Forget, Steven Magnuson, Chantal Grand-Maître, Francis Beaumier, John Liu, Lorena Riol-Blanco, Shannon D. Shields, Yong Chen, Brian Safina, Martin Dery, Elisia Villemure, Claudio Sturino, Huifen Chen, Luce Lépissier, Matthew Volgraf, Alessia Balestrini, Xiumin Wu, Daniel G. Shore, Stuart Ward, Wyne P. Lee, David H. Hackos, Andrew Peter Cridland, Robin Larouche-Gauthier, Lionel Rouge, Stephane Ciblat, Aijun Lu, Matt Baumgardner, Justin Ly, Rebecca M. Reese, Alexis Rohou, Eric Suto, Juan Zhang, Hank La
Publikováno v:
Journal of Medicinal Chemistry. 64:3843-3869
Transient receptor potential ankyrin 1 (TRPA1) is a nonselective calcium-permeable ion channel highly expressed in the primary sensory neurons functioning as a polymodal sensor for exogenous and endogenous stimuli and has generated widespread interes
Autor:
Charlotte Avet, Louis Gendron, Camil Elie Sayegh, Joseph A. Mancini, Florence Gross, Christian Le Gouill, Meriem Semache, Youssef L. Bennani, Claudio Sturino, Michel Bouvier, Sébastien Grastilleur
Publikováno v:
Communications Biology
Protease-activated receptor-2 (PAR2) is involved in inflammatory responses and pain, therefore representing a promising therapeutic target for the treatment of immune-mediated inflammatory diseases. However, as for other GPCRs, PAR2 can activate mult
Autor:
Thao Trinh, James Gillard, Clint James, Martin Duplessis, Laibin Luo, Michael Franti, Carl Thibeault, Marc-André Joly, Jessica Desjardins, Martine Brault, Claudio Sturino, Montse Llinas-Brunet, Sébastien Morin, Sonia Tremblay, Mathieu Parisien, Louie Lamorte, Josée Bordeleau, Cyrille Kuhn, François Bilodeau, Maude Poirier, Sanjay Srivastava, Christiane Yoakim, Nathalie Dansereau, James L. Gleason, Lee Fader, Vida Gorys, Louis Morency
Publikováno v:
ACS Medicinal Chemistry Letters. 7:525-530
A high-throughput screen based on a viral replication assay was used to identify inhibitors of the human cytomegalovirus. Using this approach, hit compound 1 was identified as a 4 μM inhibitor of HCMV that was specific and selective over other herpe
Autor:
Rebekah J. Carson, Pierre L. Beaulieu, Norman Aubry, Pierre R. Bonneau, Claudio Sturino, Steven R. LaPlante, René Coulombe, Gordon Bolger
Publikováno v:
Journal of Medicinal Chemistry. 56:7073-7083
A simple NMR assay was applied to monitor the tendency of compounds to self-aggregate in aqueous media. The observation of unusual spectral trends as a function of compound concentration appears to be signatory of the formation of self-assemblies. (1
Autor:
A. Pelletier, Stephen W. Mason, Daniel Rajotte, Claudio Sturino, Richard Bethell, Lise Bourgon, P. Salois, Sonia Tremblay, René Coulombe, Louie Lamorte
Publikováno v:
Antimicrobial Agents and Chemotherapy. 57:2712-2718
Several groups have recently reported on the identification of nucleotide-competing reverse transcriptase inhibitors (NcRTIs), a new class of RT inhibitors. NcRTIs reversibly inhibit binding of the incoming nucleotide to the RT active site but do not
Autor:
Clint James, Louie Lamorte, Sonia Tremblay, Joannie Minville, Alex Pelletier, Daniel Rajotte, Bruno Simoneau, Patrick Salois, Louis Morency, Michael G. Cordingley, Patrick Deroy, Jianmin Duan, Claudio Sturino, Martin Duplessis, Martin Tremblay, Teddy Halmos, Richard Bethell, Sébastien Morin, Paul J. Edwards
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:2781-2786
A HTS screen led to the identification of a benzofurano[3,2-d]pyrimidin-2-one core structure which upon further optimization resulted in 1 as a potent HIV-1 nucleotide competing reverse transcriptase inhibitor (NcRTI). Investigation of the SAR at N-1
Autor:
Yves Bousquet, Patrick Deroy, Bruno Simoneau, Joannie Minville, Louis Morency, Sébastien Morin, Martin Tremblay, Bounkham Thavonekham, Claudio Sturino, Ted Halmos, Clint James, Martin Duplessis
Publikováno v:
Tetrahedron Letters. 54:2303-2307
An efficient multi-gram synthesis of a nucleotide-competing reverse transcriptase inhibitor is reported. The synthesis features a chiral auxiliary-assisted alcohol resolution, a Mitsunobu reaction involving a carbamate, followed by a lithium-iodide e
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7440-7443
The strategy and SAR studies that led to the discovery of a novel potent and orally available 5-lipoxygenase (5-LO) inhibitor 3-(4-fluorophenyl)-6-({4-[(1S)-1-hydroxy-1-(trifluoromethyl)propyl]-1H-1,2,3-triazol-1-yl}methyl)-1-benzothiophene-2-carboxa
Publikováno v:
Tetrahedron Letters. 49:3677-3681
A general synthesis of quinolinones and benzothiazine 1,1-dioxides is presented. A series of N-phenylacrylamides and N-phenylethylenesulfonamides were studied for their ability to undergo ring closing methathesis to yield the corresponding quinolinon
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