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

…, Y Kim, S Weerasekara, M Moroze, KR Alliston…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 23 p. 6317 - 6320

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Citation Number: 19

Abstract

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, ...