Potent β-lactam inhibitors of human cytomegalovirus protease

被引：25

作者：

Yoakim, C ^{[1
]}

Ogilvie, WW ^{[1
]}

Cameron, DR ^{[1
]}

Chabot, C ^{[1
]}

Grand-Maitre, C ^{[1
]}

Guse, I ^{[1
]}

Hache, B ^{[1
]}

Kawai, S ^{[1
]}

Naud, J ^{[1
]}

O'Meara, JA ^{[1
]}

Plante, R ^{[1
]}

Deziel, R ^{[1
]}

机构：

[1] Boehringer Ingelheim Canada, Biomega Res Div, Laval, PQ H7S 2G5, Canada

来源：

ANTIVIRAL CHEMISTRY & CHEMOTHERAPY | 1998年 / 9卷 / 05期

关键词：

human cytomegalovirus; protease inhibitors; beta-lactams;

D O I：

10.1177/095632029800900502

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：379 / 387

页数：9

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