The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase.
Peptides based upon the non-prime side residues of the NS4A-4B cleavage site of hepatitis C virus (HCV) NS3-4A proteinase containing an alpha-ketoamide moiety in place of the scissile amide bond are potent inhibitors of this enzyme.
Bennett
J M
JM
Department of Chemistry, Roche Discover Welwyn, Welwyn Garden City, Hertfordshire, UK.
Campbell
A D
AD
Campbell
A J
AJ
Carr
M G
MG
Dunsdon
R M
RM
Greening
J R
JR
Hurst
D N
DN
Jennings
N S
NS
Jones
P S
PS
Jordan
S
S
Kay
P B
PB
O'Brien
M A
MA
King-Underwood
J
J
Raynham
T M
TM
Wilkinson
C S
CS
Wilkinson
T C
TC
Wilson
F X
FX
D000577:Amides / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D006801:Humans; D020128:Inhibitory Concentration 50; D018716:Molecular Mimicry; D010455:Peptides / Q000138:chemical synthesis / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors*
D000577:Amides; D000998:Antiviral Agents; C093542:NS4 protein, hepatitis C virus; D010455:Peptides; D015842:Serine Proteinase Inhibitors; D017361:Viral Nonstructural Proteins