title: Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency.
abstract: Modification of the P(2) and P(1) side chains of earlier P(3)-capped alpha-ketoamide inhibitor of HCV NS3 serine protease 1 resulted in the discovery of compound 24 with about 10-fold improvement in potency.
authors.affiliation: Chemical Research, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. stephane.bogen@spcorp.com
authors.forename: S
authors.initials: S
authors.lastname: Bogen
authors.forename: A K
authors.initials: AK
authors.lastname: Saksena
authors.forename: A
authors.initials: A
authors.lastname: Arasappan
authors.forename: H
authors.initials: H
authors.lastname: Gu
authors.forename: F G
authors.initials: FG
authors.lastname: Njoroge
authors.forename: V
authors.initials: V
authors.lastname: Girijavallabhan
authors.forename: J
authors.initials: J
authors.lastname: Pichardo
authors.forename: N
authors.initials: N
authors.lastname: Butkiewicz
authors.forename: A
authors.initials: A
authors.lastname: Prongay
authors.forename: V
authors.initials: V
authors.lastname: Madison
mesh_terms: D000409:Alanine / Q000737:chemistry*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry* / 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: D000409:Alanine; 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