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Comparative Study
. 2000 Jan 3;10(1):45-8.
doi: 10.1016/s0960-894x(99)00587-9.

Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors

P S Dragovich  1 , R Zhou, S E Webber, T J Prins, A K Kwok, K Okano, S A Fuhrman, L S Zalman, F C Maldonado, E L Brown, J W Meador 3rd, A K Patick, C E Ford, M A Brothers, S L Binford, D A Matthews, R A Ferre, S T Worland
Affiliations
Comparative Study

Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors

P S Dragovich et al. Bioorg Med Chem Lett. .

Abstract

Tripeptide-derived molecules incorporating C-terminal ketone electrophiles were evaluated as reversible inhibitors of the cysteine-containing human rhinovirus 3C protease (3CP). An optimized example of such compounds displayed potent 3CP inhibition activity (K = 0.0045 microM) and in vitro antiviral properties (EC50=0.34 microM) when tested against HRV serotype-14.

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