Smith D G, Gribble A D, Haigh D, Ife R J, Lavery P, Skett P, Slingsby B P, Stacey R, Ward R W, West A
SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.
Bioorg Med Chem Lett. 1999 Nov 1;9(21):3137-42. doi: 10.1016/s0960-894x(99)00539-9.
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 Ser132 whereas non-oxazinone derived hydroxylamines appear to inhibit via formation of a sulfinanilide at Cys138.
已经合成了芳基羟胺衍生物，它们是迄今为止制备的最有效的人巨细胞病毒蛋白酶抑制剂中的一些（IC50为14 - 60 nM）。质谱研究表明，恶嗪酮衍生的羟胺通过酰化Ser132来抑制该酶，而非恶嗪酮衍生的羟胺似乎是通过在Cys138处形成亚磺酰苯胺来抑制。
