Bioorganic and Medicinal Chemistry Letters p. 2683 - 2686 (2001)
Update date:2022-09-26
Topics:
Webber, Stephen E.
Marakovits, Joseph T.
Dragovich, Peter S.
Prins, Thomas J.
Zhou, Ru
Fuhrman, Shella A.
Patick, Amy K.
Matthews, David A.
Lee, Caroline A.
Srinivasan, Babu
Moran, Terry
Ford, Clifford E.
Brothers, Mary A.
Harr, James E.V.
Meador III, James W.
Ferre, Rose Ann
Worland, Stephen T.
Novel tripeptidyl C-terminal Michael acceptors with an ester replacement of the P2-P3 amide bond were investigated as irreversible inhibitors of the human rhinovirus (HRV) 3C protease (3CP). When screened against HRV serotype-14 the best compound was shown to have very good 3CP inhibition (kobs/[I]=270,000 M-1 s-1) and potent in vitro antiviral activity (EC50=7.0 nM).
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