title: P2-P4 macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease.
abstract: Synthesis and HCV NS3 serine protease inhibitory activity of 4-hydroxyproline derived macrocyclic inhibitors and SAR around this macrocyclic core is described in this communication. X-ray structure of inhibitor 38 bound to the protease is discussed.
authors.affiliation: Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. ashok.arasappan@spcorp.com
authors.forename: Ashok
authors.initials: A
authors.lastname: Arasappan
authors.forename: F George
authors.initials: FG
authors.lastname: Njoroge
authors.forename: Kevin X
authors.initials: KX
authors.lastname: Chen
authors.forename: Srikanth
authors.initials: S
authors.lastname: Venkatraman
authors.forename: Tejal N
authors.initials: TN
authors.lastname: Parekh
authors.forename: Haining
authors.initials: H
authors.lastname: Gu
authors.forename: John
authors.initials: J
authors.lastname: Pichardo
authors.forename: Nancy
authors.initials: N
authors.lastname: Butkiewicz
authors.forename: Andrew
authors.initials: A
authors.lastname: Prongay
authors.forename: Vincent
authors.initials: V
authors.lastname: Madison
authors.forename: Viyyoor
authors.initials: V
authors.lastname: Girijavallabhan
mesh_terms: D006526:Hepatitis C / Q000201:enzymology*; D047028:Macrocyclic Compounds / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000494:pharmacology*; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*; D014961:X-Ray Diffraction; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases
chemical_list: D047028:Macrocyclic Compounds; D015842:Serine Proteinase Inhibitors; D017361:Viral Nonstructural Proteins; C084422:NS3 protein, hepatitis C virus; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases