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

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Issue Date
2013-12-01
Authors
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.
Advisor
Citation

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. 2013. Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors. Bioorganic & Medicinal Chemistry Letters, vol. 23:no. 23:pp. 6317-6320, 1 December 2013

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, a-ketoamide, bisulfite adduct, and a-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.

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