Cyclic sulfones as novel P3-caps for hepatitis C virus NS3/4A (HCV NS3/4A) protease inhibitors: synthesis and evaluation of inhibitors with improved potency and pharmacokinetic profiles.
Velázquez
Francisco
F
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033-1300, USA. francisco.velazquez@spcorp.com
Sannigrahi
Mousumi
M
Bennett
Frank
F
Lovey
Raymond G
RG
Arasappan
Ashok
A
Bogen
Stéphane
S
Nair
Latha
L
Venkatraman
Srikanth
S
Blackman
Melissa
M
Hendrata
Siska
S
Huang
Yuhua
Y
Huelgas
Regina
R
Pinto
Patrick
P
Cheng
Kuo-Chi
KC
Tong
Xiao
X
McPhail
Andrew T
AT
Njoroge
F George
FG
D000284:Administration, Oral; D000818:Animals; D018360:Crystallography, X-Ray; D000882:Haplorhini; D016174:Hepacivirus / Q000201:enzymology*; D008958:Models, Molecular; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
C549336:N-(1-(2-(cyclopropylamino)-1,2-dioxoethyl)butyl)-6,6-dimethyl-3-(2-(1-methylcyclohexyl)-2-((((1-(tetrahydro-1,1-dioxido-2-thienyl)cyclohexyl)amino)carbonyl)amino)acetyl)-3-azabicyclo(3.1.0)hexane-2-carboxamide; C549335:N-(1-(2-(cyclopropylamino)-1,2-dioxoethyl)pentyl)-6,6-dimethyl-3-(2-(1-methylcyclohexyl)-2-((((1-(tetrahydro-1,1-dioxido-2-thienyl)cyclohexyl)amino)carbonyl)amino)acetyl)-3-azabicyclo(3.1.0)hexane-2-carboxamide; D009842:Oligopeptides; D015842:Serine Proteinase Inhibitors; D013450:Sulfones