title: SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease.
abstract: SAR on the phenethylamide 1 (Ki 1.2 microM) in the P2- and the P'-position led to potent inhibitors, one of which showed good exposure and low clearance when administered intramuscularly to rat.
authors.affiliation: Department of Chemistry, Istituto di Ricerche di Biologia Molecolare, Merck Research Laboratories, Via Pontina Km 30.600, 00040 Pomezia, Rome, Italy.
authors.forename: Savina
authors.initials: S
authors.lastname: Malancona
authors.forename: Stefania
authors.initials: S
authors.lastname: Colarusso
authors.forename: Jesus M
authors.initials: JM
authors.lastname: Ontoria
authors.forename: Antonella
authors.initials: A
authors.lastname: Marchetti
authors.forename: Marco
authors.initials: M
authors.lastname: Poma
authors.forename: Ian
authors.initials: I
authors.lastname: Stansfield
authors.forename: Ralph
authors.initials: R
authors.lastname: Laufer
authors.forename: Annalise
authors.initials: A
authors.lastname: Di Marco
authors.forename: Marina
authors.initials: M
authors.lastname: Taliani
authors.forename: Maria
authors.initials: M
authors.lastname: Verdirame
authors.forename: Odalys
authors.initials: O
authors.lastname: Gonzalez-Paz
authors.forename: Victor G
authors.initials: VG
authors.lastname: Matassa
authors.forename: Frank
authors.initials: F
authors.lastname: Narjes
mesh_terms: D000818:Animals; D016174:Hepacivirus / Q000187:drug effects / Q000201:enzymology*; D010627:Phenethylamines / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D012697:Serine Endopeptidases / Q000493:pharmacokinetics*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors* / Q000493:pharmacokinetics*; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases
chemical_list: D010627:Phenethylamines; 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; C093542:NS4 protein, hepatitis C virus