title: Discovery of a novel bicycloproline P2 bearing peptidyl alpha-ketoamide LY514962 as HCV protease inhibitor.
abstract: We describe herein the design, syntheses and evaluation of a number of bicycloproline P2 bearing HCV protease inhibitors endowed with impressive enzyme potency, enzyme selectivity, cellular activity and favorable ADME profiles.
authors.affiliation: Lilly Research Laboratory, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
authors.forename: Yvonne
authors.initials: Y
authors.lastname: Yip
authors.forename: Frantz
authors.initials: F
authors.lastname: Victor
authors.forename: Jason
authors.initials: J
authors.lastname: Lamar
authors.forename: Robert
authors.initials: R
authors.lastname: Johnson
authors.forename: Q May
authors.initials: QM
authors.lastname: Wang
authors.forename: Donna
authors.initials: D
authors.lastname: Barket
authors.forename: John
authors.initials: J
authors.lastname: Glass
authors.forename: Ling
authors.initials: L
authors.lastname: Jin
authors.forename: Lifei
authors.initials: L
authors.lastname: Liu
authors.forename: Daryl
authors.initials: D
authors.lastname: Venable
authors.forename: Mark
authors.initials: M
authors.lastname: Wakulchik
authors.forename: Congping
authors.initials: C
authors.lastname: Xie
authors.forename: Beverly
authors.initials: B
authors.lastname: Heinz
authors.forename: Elcira
authors.initials: E
authors.lastname: Villarreal
authors.forename: Joe
authors.initials: J
authors.lastname: Colacino
authors.forename: Nathan
authors.initials: N
authors.lastname: Yumibe
authors.forename: Mark
authors.initials: M
authors.lastname: Tebbe
authors.forename: John
authors.initials: J
authors.lastname: Munroe
authors.forename: Shu-Hui
authors.initials: SH
authors.lastname: Chen
mesh_terms: D000818:Animals; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D004151:Dipeptides / Q000138:chemical synthesis / Q000494:pharmacology; D016174:Hepacivirus / Q000187:drug effects* / Q000201:enzymology; D006801:Humans; D008297:Male; D011392:Proline / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D012697:Serine Endopeptidases / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D017361:Viral Nonstructural Proteins / Q000378:metabolism*; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases
chemical_list: D001643:Bridged Bicyclo Compounds; D004151:Dipeptides; D011392:Proline; D012697:Serine Endopeptidases; D015842:Serine Proteinase Inhibitors; D017361:Viral Nonstructural Proteins; C084422:NS3 protein, hepatitis C virus; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases