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

Autor: Prior AM; Department of Chemistry, Kansas State University, 213 CBC Building, Manhattan, KS 66506, United States., Kim Y, Weerasekara S, Moroze M, Alliston KR, Uy RA, Groutas WC, Chang KO, Hua DH
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Dec 01; Vol. 23 (23), pp. 6317-20. Date of Electronic Publication: 2013 Sep 30.
DOI: 10.1016/j.bmcl.2013.09.070
Abstrakt: 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.
(Copyright © 2013 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE