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  • Title: Phosphonate inhibitors of West Nile virus NS2B/NS3 protease.
    Author: Skoreński M, Milewska A, Pyrć K, Sieńczyk M, Oleksyszyn J.
    Journal: J Enzyme Inhib Med Chem; 2019 Dec; 34(1):8-14. PubMed ID: 30362835.
    Abstract:
    West Nile virus (WNV) is a member of the flavivirus genus belonging to the Flaviviridae family. The viral serine protease NS2B/NS3 has been considered an attractive target for the development of anti-WNV agents. Although several NS2B/NS3 protease inhibitors have been described so far, most of them are reversible inhibitors. Herein, we present a series of α-aminoalkylphosphonate diphenyl esters and their peptidyl derivatives as potent inhibitors of the NS2B/NS3 protease. The most potent inhibitor identified was Cbz-Lys-Arg-(4-GuPhe)P(OPh)2 displaying Ki and k2/Ki values of 0.4 µM and 28 265 M-1s-1, respectively, with no significant inhibition of trypsin, cathepsin G, and HAT protease.
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