2-chloro-3-substituted-1,4-naphthoquinone inactivators of human cytomegalovirus protease.
A random screening approach has identified 2-chloro-3-substituted-1,4-naphthoquinones as potent inactivators of HCMV protease. Enzyme inactivation is due to modification of Cys202. Two of the most potent compounds maintain activity against HCMV in a plaque reduction assay.
Ertl
P
P
GlaxoWellcome Medicines Research Centre, Stevenage, UK.
Cooper
D
D
Allen
G
G
Slater
M J
MJ
D001665:Binding Sites; D002460:Cell Line; D003545:Cysteine / Q000737:chemistry; D005978:Glutathione / Q000737:chemistry; D006801:Humans; D019272:Leukocyte Elastase / Q000378:metabolism; D015394:Molecular Structure; D009285:Naphthoquinones / Q000138:chemical synthesis* / Q000494:pharmacology; D012697:Serine Endopeptidases / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013917:Thrombin / Q000378:metabolism; D010948:Viral Plaque Assay
D009285:Naphthoquinones; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; C071910:assemblin; D019272:Leukocyte Elastase; D013917:Thrombin; D005978:Glutathione; D003545:Cysteine; C035342:1,4-naphthoquinone