Aryl hydroxylamine derivs. have been synthesized that are some of the most potent inhibitors of hCMV protease prepd. 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.
|Number of pages||6|
|Journal||Bioorganic & Medicinal Chemistry Letters|
|Publication status||Published - 01 Nov 1999|
ASJC Scopus subject areas
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
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. (1999). The inhibition of human cytomegalovirus (hCMV) protease by hydroxylamine derivatives. Bioorganic & Medicinal Chemistry Letters, 9(21)(21), 3137-3142.