Zobrazeno 1 - 10
of 41
pro vyhledávání: '"Pierre R. Bonneau"'
Autor:
Steven R. LaPlante, René Coulombe, Thao Trinh, Dominik Wernic, Rebekah J. Carson, Nathalie Rioux, Bruno Simoneau, Catherine Chabot, Youla S. Tsantrizos, Jianmin Duan, Simon Surprenant, Pierre R. Bonneau, Carl Thibeault, Stephen W. Mason, Serge Landry, Craig Fenwick, François Bilodeau, Araz Jakalian, Murray D. Bailey, Stephen H. Kawai, Clint James, Yves Bousquet, Bounkham Thavonekham, Michel Garneau, Eric Beaulieu, Sébastien Morin, Christiane Yoakim, Ted Halmos, Lee Fader, Jennifer Tsoung
Publikováno v:
ACS Medicinal Chemistry Letters. 7:797-801
Optimization of pyridine-based noncatalytic site integrase inhibitors (NCINIs) based on compound 2 has led to the discovery of molecules capable of inhibiting virus harboring N124 variants of HIV integrase (IN) while maintaining minimal contribution
Autor:
Nathalie Rioux, Sonia Tremblay, Michel Garneau, Pierre R. Bonneau, René Coulombe, Marc-André Poupart, Bruno Simoneau, Steve Mason, Louie Lamorte, Patricia Schroeder, Stephen H. Kawai, Jianmin Duan, Ma’an Amad, Laibin Luo, Lee Fader, Anne-Marie Faucher, Steven R. LaPlante, Craig Fenwick, Araz Jakalian, Michael Bös, Youla S. Tsantrizos, Paul J. Edwards, Myriam Witvrouw, Murray D. Bailey, Michael G. Cordingley, Richard Bethell, Christiane Yoakim
Publikováno v:
Antimicrobial Agents and Chemotherapy. 58:3233-3244
BI 224436 is an HIV-1 integrase inhibitor with effective antiviral activity that acts through a mechanism that is distinct from that of integrase strand transfer inhibitors (INSTIs). This 3-quinolineacetic acid derivative series was identified using
Autor:
Marc Pesant, Christian Brochu, Rebekah J. Carson, Bruno Simoneau, Patricia Schroeder, Murray D. Bailey, Pierre R. Bonneau, Michael G. Cordingley, Catherine Chabot, Michel Garneau, Anne-Marie Faucher, Michael Bös, René Coulombe, Mathieu Parisien, Stephen W. Mason, Araz Jakalian, Jianmin Duan, Marc-André Poupart, Dominik Wernic, Sébastien Morin, François Bilodeau, Serge Landry, Yves Bousquet, Eric Malenfant, Stephen H. Kawai, Punit Bhardwaj, Ma’an Amad, Lee Fader, Youla S. Tsantrizos, Richard Bethell, Christiane Yoakim, Steven R. LaPlante, Paul J. Edwards, Ted Halmos, Craig Fenwick
Publikováno v:
ACS Medicinal Chemistry Letters. 5:422-427
An assay recapitulating the 3' processing activity of HIV-1 integrase (IN) was used to screen the Boehringer Ingelheim compound collection. Hit-to-lead and lead optimization beginning with compound 1 established the importance of the C3 and C4 substi
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:
Rebekah J. Carson, Sylvain Bordeleau, Michael J. Little, Pierre L. Beaulieu, Steven R. LaPlante, Jeff A. O'Meara, James Gillard, Pierre R. Bonneau, Norman Aubry, René Coulombe
Publikováno v:
Journal of Medicinal Chemistry. 56:5142-5150
The pharmaceutical industry has recognized that many drug-like molecules can self-aggregate in aqueous media and have physicochemical properties that skew experimental results and decisions. Herein, we introduce the use of a simple NMR strategy for d
Autor:
Stephen W. Mason, Bruno Simoneau, Oliver Hucke, Sébastien Morin, Yves Bousquet, Jianmin Duan, Steve Titolo, Serge Landry, Isabelle Dion, Michel Garneau, Christopher T. Lemke, Pierre R. Bonneau, Lee Fader, Stephen H. Kawai, Sylvie Goulet, Nathalie Goudreau, Jean Rancourt, Ma’an Amad
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3401-3405
Detailed structure–activity relationships of the C3-phenyl moiety that allow for the optimization of antiviral potency of a series of 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione inhibitors of HIV capsid (CA) assembly are described. Combination of f
Autor:
Michel Garneau, Jianmin Duan, Hao Zhu, Pierre R. Bonneau, Denis Fourches, Alexander Sedykh, Oliver Hucke, Alexander Tropsha
Publikováno v:
Pharmaceutical Research. 30:996-1007
Membrane transporters mediate many biological effects of chemicals and play a major role in pharmacokinetics and drug resistance. The selection of viable drug candidates among biologically active compounds requires the assessment of their transporter
Autor:
Bruno Simoneau, Oliver Hucke, Ingrid Guse, Martin Duplessis, Alexandre Gagnon, Yves Bousquet, Patrick Deroy, Jianmin Duan, Martin Tremblay, Christopher T. Lemke, Pierre R. Bonneau, Stephen W. Mason, Steve Titolo, Nathalie Goudreau, Stephen H. Kawai, Simon Surprenant, Michel Garneau, Christiane Yoakim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7512-7517
A uHTS campaign led to the discovery of a 5-(5-furan-2-ylpyrazol-1-yl)-1H-benzimidazole series that inhibits assembly of HIV-1 capsid. Synthetic manipulations at N1, C2 and C16 positions improved the antiviral potency by a . The X-ray structure of 33
Autor:
Jeff A. O'Meara, Alexandre Gagnon, Sébastien Morin, Serge Landry, Michael Bös, Patrick Deroy, Christopher T. Lemke, Pierre R. Bonneau, Steve Titolo, Yves Bousquet, Stephen W. Mason, Bruno Simoneau, Eric Malenfant, Oliver Hucke, René Coulombe, Ingrid Guse, Richard Bethell, Chantal Grand-Maître, Anne-Marie Faucher, Jean-Eric Lacoste, Christiane Yoakim, Michael G. Cordingley, Stephen H. Kawai, Nathalie Goudreau, Lee Fader
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:398-404
The discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly is described. Synthesis of analogs of the 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione hit established structure-activity relationships. Repla
Autor:
Alexandre Gagnon, René Coulombe, Michel Garneau, Araz Jakalian, Patrick Deroy, Bruno Simoneau, Jianmin Duan, Serge Landry, Eric Jolicoeur, Christiane Yoakim, Pierre R. Bonneau, Louise Doyon, Ingrid Guse, Eric Malenfant, Ma’an Amad
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4437-4441
A series of aryl thiotetrazolylacetanilides were synthesized and found to be potent inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases. The incorporation of an alkynyl fragment on the aniline provided inhibitors wi