Inhibition of herpes proteases and antiviral activity of 2-substituted thieno[2,3-d]oxazinones.
Cinnamyl derivatives of thieno[2,3-d]oxazinones are mechanism-based inhibitors of the HSV-2, VZV and CMV herpes proteases which demonstrate nanomolar potency. Compounds 5 and 28 inhibit protease processing in HSV-2 infected cells with a selectivity index of at least 30.
Jarvest
R L
RL
SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK. Richard_L_Jarvest@sbphrd.com
Pinto
I L
IL
Ashman
S M
SM
Dabrowski
C E
CE
Fernandez
A V
AV
Jennings
L J
LJ
Lavery
P
P
Tew
D G
DG
D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D006564:Herpesviridae / Q000201:enzymology*; D010078:Oxazines / Q000737:chemistry / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology*
D000998:Antiviral Agents; D010078:Oxazines; D011480:Protease Inhibitors