The inhibition of human cytomegalovirus (hCMV) protease by hydroxylamine derivatives

被引:17
作者
Smith, DG [1 ]
Gribble, AD [1 ]
Haigh, D [1 ]
Ife, RJ [1 ]
Lavery, P [1 ]
Skett, P [1 ]
Slingsby, BP [1 ]
Stacey, R [1 ]
Ward, RW [1 ]
West, A [1 ]
机构
[1] SmithKline Beecham Pharmaceut, Harlow CM19 5AW, Essex, England
关键词
D O I
10.1016/S0960-894X(99)00539-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Aryl hydroxylamine derivatives have been synthesised that are some of the most potent inhibitors of hCMV protease prepared to date (IC50 14-60 nM). Mass spectrometry studies indicate that oxazinone derived hydroxylamines inhibit the enzyme by acylation of Ser(132) whereas non-oxazinone derived hydroxylamines appear to inhibit via formation of a sulfinanilide at Cys(138). (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3137 / 3142
页数:6
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