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Eric Malenfant
Researcher at Boehringer Ingelheim
Publications - 30
Citations - 883
Eric Malenfant is an academic researcher from Boehringer Ingelheim. The author has contributed to research in topics: Reagent & Enantioselective synthesis. The author has an hindex of 17, co-authored 30 publications receiving 829 citations.
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Journal ArticleDOI
Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.
Lee Fader,Eric Malenfant,Mathieu Parisien,Rebekah J. Carson,François Bilodeau,Serge Landry,Marc Pesant,Christian Brochu,Sébastien Morin,Catherine Chabot,Ted Halmos,Yves Bousquet,Murray D. Bailey,Stephen H. Kawai,René Coulombe,Steven R. LaPlante,Araz Jakalian,Punit Bhardwaj,Dominik Wernic,Patricia Schroeder,Ma’an Amad,Paul J. Edwards,Michel Garneau,Jianmin Duan,Michael G. Cordingley,Richard Bethell,Stephen W. Mason,Michael Bös,Pierre R. Bonneau,Marc-André Poupart,Anne-Marie Faucher,Bruno Simoneau,Craig Fenwick,Christiane Yoakim,Youla S. Tsantrizos +34 more
TL;DR: An assay recapitulating the 3' processing activity of HIV-1 integrase (IN) was used to screen the Boehringer Ingelheim compound collection, leading to the discovery of compound 26 (BI 224436), the first NCINI to advance into a phase Ia clinical trial.
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Discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly
Lee Fader,Richard Bethell,Pierre R. Bonneau,Michael Bös,Yves Bousquet,Michael G. Cordingley,René Coulombe,Patrick Deroy,Anne-Marie Faucher,Alexandre Gagnon,Nathalie Goudreau,Chantal Grand-Maître,Ingrid Guse,Oliver Hucke,Stephen H. Kawai,Jean-Eric Lacoste,Serge Landry,Christopher T. Lemke,Eric Malenfant,Stephen W. Mason,Sébastien Morin,Jeff A. O'Meara,Bruno Simoneau,Steve Titolo,Christiane Yoakim +24 more
TL;DR: Replacement of the enamine functionality of the hit series with either an imidazole or a pyrazole ring led to compounds that inhibited both capsid assembly and reverse transcriptase, leading to lead compound 48, a pure capsidAssembly inhibitor with improved antiviral activity.
Journal ArticleDOI
Asymmetric Ring Closure Reactions Mediated by a Chiral C2 Symmetrical Organoselenium Reagent
Robert Deziel,Eric Malenfant +1 more
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Inhibition of Human Cytomegalovirus Protease by Monocyclic β-Lactam Derivatives: Kinetic Characterization Using a Fluorescent Probe
Pierre R. Bonneau,Firoz Hasani,Céline Plouffe,Eric Malenfant,Steve R. LaPlante,Ingrid Guse,William W. Ogilvie,Raymond Plante,Walter Davidson,Jerry L. Hopkins,Maurice M. Morelock,and Michael G. Cordingley,Robert Deziel +12 more
TL;DR: Examination of a series of progress curves by numerical analysis has provided valuable information on acylation and deacylation rates which relate to the IC50 values observed for β-lactams.
Journal ArticleDOI
2,6-Bis[(2S)-tetrahydrofuran-2-yl]phenyl diselenide: An effective reagent for asymmetric electrophilic addition reactions to olefins
TL;DR: The enantioselective synthesis of a new and extremely effective organoselenium reagent (2 ) is reported in this paper, which was found to react with alkenes with a very high degree of facial selectivity in selenomethoxylation and ring closure reactions.