| Title | Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors. | ||
| Author | Prior, Allan M; Kim, Yunjeong; Weerasekara, Sahani; Moroze, Meghan; Alliston, Kevin R; Uy, Roxanne Adeline Z; Groutas, William C; Chang, Kyeong-Ok; Hua, Duy H | ||
| Journal | Bioorg Med Chem Lett | Publication Year/Month | 2013-Dec |
| PMID | 24125888 | PMCID | PMC3863581 |
| Affiliation | 1.Department of Chemistry, Kansas State University, 213 CBC Building, Manhattan, KS 66506, United States. | ||
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, alpha-ketoamide, bisulfite adduct, and alpha-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.