Yoakim C, Ogilvie W W, Cameron D R, Chabot C, Grand-Maître C, Guse I, Haché B, Kawai S, Naud J, O'Meara J A, Plante R, Déziel R
Bio-Méga Research Division, Boehringer Ingelheim (Canada), Laval, Québec.
Antivir Chem Chemother. 1998 Sep;9(5):379-87. doi: 10.1177/095632029800900502.
A series of novel monobactam inhibitors of human cytomegalovirus (HCMV) protease has been described that possess a heterocyclic thiomethyl side chain at C-4. Changes to the heterocycle did not significantly change the inhibitory activity of these compounds in an enzymatic assay, although improvements in solubility and cell culture activity were noted. A number of permutations between C-4 substitutions and N-1 derivatives led to the identification of several beta-lactams with antiviral activity in a plaque reduction assay. N-methyl thiotetrazole-containing compounds were found to be the most potent inhibitors in the enzymatic assay.
已描述了一系列新型的人巨细胞病毒（HCMV）蛋白酶单环β-内酰胺抑制剂，这些抑制剂在C-4位具有杂环硫甲基侧链。尽管观察到溶解性和细胞培养活性有所改善，但杂环的改变在酶促试验中并未显著改变这些化合物的抑制活性。C-4取代基与N-1衍生物之间的多种排列组合导致在蚀斑减少试验中鉴定出几种具有抗病毒活性的β-内酰胺。在酶促试验中发现含N-甲基硫代四唑的化合物是最有效的抑制剂。
