Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors.

ABSTRACT: A class of tripeptidyl transition state inhibitors containing a P1 glutamine surrogate, a P2 leucine, and a P3 arylalanines, was found to potently inhibit Norwalk virus replication in enzyme and cell based assays. An array of warheads, including aldehyde, α-ketoamide, bisulfite adduct, and α-hydroxyphosphonate transition state mimic, was also investigated. Tripeptidyls 2 and 6 possess antiviral activities against noroviruses, human rhinovirus, severe acute respiratory syndrome coronavirus, and coronavirus 229E, suggesting a broad range of antiviral activities.

SUBMITTER: Prior AM 

PROVIDER: S-EPMC3863581 | biostudies-literature | 2013 Dec

REPOSITORIES: biostudies-literature