SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease

The development of phenethylamide 23 ( K i 0.1 μM) is described together with the pharmacokinetics behavior of this and related compounds. SAR on the phenethylamide 1 ( K i 1.2 μM) in the P2- and the P′-position led to potent inhibitors, one of which showed good exposure and low clearance when admin...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-09, Vol.14 (17), p.4575-4579
Hauptverfasser:	Malancona, Savina, Colarusso, Stefania, Ontoria, Jesus M, Marchetti, Antonella, Poma, Marco, Stansfield, Ian, Laufer, Ralph, Di Marco, Annalise, Taliani, Marina, Verdirame, Maria, Gonzalez-Paz, Odalys, Matassa, Victor G, Narjes, Frank
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Hepacivirus - drug effects Hepacivirus - enzymology Medical sciences Miscellaneous Pharmacology. Drug treatments Phenethylamines - chemistry Phenethylamines - pharmacology Rats Serine Endopeptidases - pharmacokinetics Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - pharmacology Structure-Activity Relationship Viral Nonstructural Proteins - antagonists & inhibitors Viral Nonstructural Proteins - pharmacokinetics
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Zusammenfassung:	The development of phenethylamide 23 ( K i 0.1 μM) is described together with the pharmacokinetics behavior of this and related compounds. SAR on the phenethylamide 1 ( K i 1.2 μM) 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.05.093