Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Sebastien Laliberte"'
Autor:
Christian Salesse, Habib Horchani, Sylvain Bussières, Jean-Sebastien Laliberte-Gemme, Rock Breton, Line Cantin, Mustapha Lhor
Publikováno v:
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics. 1844:1128-1136
Lecithin retinol acyltransferase (LRAT) plays a major role in the vertebrate visual cycle. Indeed, it is responsible for the esterification of all-trans retinol into all-trans retinyl esters, which can then be stored in microsomes or further metaboli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1053de328b95245c8a324dc9bea0308b
https://doi.org/10.1016/j.bbapap.2014.02.022
https://doi.org/10.1016/j.bbapap.2014.02.022
Autor:
Kelly Bleasby, Dwight Macdonald, Bruce Mackay, Richard Tschirret-Guth, Robert Houle, Sebastien Laliberte, Patrick Lacombe, Robert Papp, Erich L. Grimm, Amandine Chefson, Jean-François Lévesque, Michael J. Hafey, Pierre-André Fournier, Sébastien Gagné, Yongxin Han, Yves Ducharme, Michel Gallant, Austin Chen, Daniel Dube
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5547-5551
An oral bioavailability issue encountered during the course of lead optimization in the renin program is described herein. The low F(po) of pyridone analogs was shown to be caused by a combination of poor passive permeability and gut efflux transport
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2b390428a9f09b127996a8190fb39ae
https://doi.org/10.1016/j.bmcl.2011.06.095
https://doi.org/10.1016/j.bmcl.2011.06.095
Autor:
Stephen M. Soisson, Tom Y.-H. Wu, Michel Gallant, Austin Chen, Dwight Macdonald, Daniel Dube, Robert Houle, Jean-Pierre Falgueyret, Renee Aspiotis, Dan McKay, Jean-François Lévesque, Patrick Roy, Helene Juteau, Sébastien Gagné, M. David Percival, Erich L. Grimm, Sebastien Laliberte, Patrick Lacombe, Elizabeth Cauchon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2430-2436
The incorporation of a carboxylic acid within in a series of 3-amido-4-aryl substituted piperidines (represented by general structure 32) led to the discovery of potent, zwitterionic, renin inhibitors with improved off-target profiles (CYP3A4 time-de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5869451b5d4a9f35f5a8af8a027ba80
https://doi.org/10.1016/j.bmcl.2011.02.067
https://doi.org/10.1016/j.bmcl.2011.02.067
Publikováno v:
Tetrahedron Letters. 51:363-366
The synthesis of pyrazino[1,2-a]indoles via a palladium-catalyzed double allylic alkylation of indole-2-hydroxamates is described. The reaction conditions are very mild and allow for a wide variety of substitutions on the indole core.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e6315a84e0d83ade20a883a48262d88e
https://doi.org/10.1016/j.tetlet.2009.11.031
https://doi.org/10.1016/j.tetlet.2009.11.031
Autor:
Renee Aspiotis, Amadine Chefson, Jean-François Lévesque, Yongxin Han, Louis-Charles Campeau, Dan McKay, Guillaume Larouche, Jean-Pierre Falgueyret, Robert Houle, Elizabeth Cauchon, David Percival, Austin Chen, Sébastien Gagné, Yves Ducharme, Sebastien Laliberte
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(24)
The discovery and SAR of a novel series of spirocyclic renin inhibitors are described herein. It was found that by restricting the northern aromatic plate to the bioactive conformation through spirocyclization, increase in renin potency and decrease
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14e96c2b9e806e5f34e8d01ee0f1bb22
https://pubmed.ncbi.nlm.nih.gov/22071301
https://pubmed.ncbi.nlm.nih.gov/22071301
Autor:
Paul Krolikowski, Kevin P. Bateman, Cheri M Maciolek, Sebastien Laliberte, Bennett Ma, Karsten Menzel, Christopher R. Gibson
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 39(5)
Setileuton [4-(4-fluorophenyl)-7-[({5-[(1S)-1-hydroxy-1-(trifluoromethyl)propyl]-1,3,4-oxadiazol-2-yl}amino)methyl]-2H-1-benzopyran-2-one] is a selective inhibitor of the 5-lipoxygenase enzyme, which is under investigation for the treatment of asthma
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86cd61695a744d622d67d650ef50e2d3
https://pubmed.ncbi.nlm.nih.gov/21325431
https://pubmed.ncbi.nlm.nih.gov/21325431
Autor:
Christopher P. Regan, Elizabeth Cauchon, Bruce Mackay, Yves Ducharme, Sylvie Toulmond, Sebastien Laliberte, Patrick Lacombe, Sébastien Gagné, M. David Percival, Daniel Dube, Jean-Pierre Falgueyret, JingQi Huang, Jean-François Lévesque, Dan McKay, Yongxin Han, René St-Jacques, Louis-Charles Campeau, Austin Chen, Hillary K. Regan, Pierre-André Fournier, Amandine Chefson, Erich L. Grimm, Robert Houle, Dwight Macdonald, Susana Liu
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(13)
An SAR campaign aimed at decreasing the overall lipophilicity of renin inhibitors such as 1 is described herein. It was found that replacement of the northern appendage in 1 with an N-methyl pyridone and subsequent re-optimization of the benzyl amide
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6984bb7f944791450d3c0856db18d4c4
https://pubmed.ncbi.nlm.nih.gov/21621998
https://pubmed.ncbi.nlm.nih.gov/21621998
Autor:
Laurence Dube, Richard Friesen, Karen Townson, Daniel Dube, Jean-François Lévesque, Susana Liu, Michel Gallant, Dwight Macdonald, Donald W. Nicholson, Zheng Huang, Renee Aspiotis, Rebecca Dias, Sebastien Laliberte, Patrick Lacombe, Pierre Hamel, Daniel Guay, Kerry A. Waters, Mario Girard, Joseph A. Mancini, Stephen Day, Robert N. Young, Angela Styhler, Yves Girard
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(22)
The structure-activity relationship of a novel series of 8-biarylnaphthyridinones acting as type 4 phosphodiesterase (PDE4) inhibitors for the treatment of long-term memory loss and mild cognitive impairment is described herein. The manuscript descri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2255fde5f2d2efbe35673f8b5806fa8e
https://pubmed.ncbi.nlm.nih.gov/20933411
https://pubmed.ncbi.nlm.nih.gov/20933411
Autor:
Laurence Dube, David Martin, Daniel Dube, Dan McKay, Michel Gallant, Robert Houle, Austin Chen, Dwight Macdonald, Bruce Mackay, Erich L. Grimm, Suzanna Liu, Sebastien Laliberte, Patrick Lacombe, Sébastien Gagné, David A. Powell, Mireille Gaudreault, Jean-François Lévesque
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(17)
Time-dependent inhibitors of CYPs have the potential to perpetrate drug-drug interactions in the clinical setting. After finding that several leading compounds in a novel series of substituted amino propanamide renin inhibitors inactivated CYP3A4 in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f193309cdedef2ef1eb3b94189c04f54
https://pubmed.ncbi.nlm.nih.gov/20673718
https://pubmed.ncbi.nlm.nih.gov/20673718
Publikováno v:
ChemInform. 41
The synthesis of pyrazino[1,2-a]indoles via a palladium-catalyzed double allylic alkylation of indole-2-hydroxamates is described. The reaction conditions are very mild and allow for a wide variety of substitutions on the indole core.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8589ddb426726a96a4126fa807f6b9b2
https://doi.org/10.1002/chin.201017172
https://doi.org/10.1002/chin.201017172