Synthesis, activity and structure–activity relationship of noroviral protease inhibitors†
Abstract
The protease of norovirus, an important human pathogen, is essential for the viral replication and, therefore, represents a potential drug target. A series of tripeptide-based inhibitors of the protease were designed, synthesized and tested, among which several potent inhibitors were identified with Ki values as low as 75 nM. The structure–activity relationships of these inhibitors are discussed.