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Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors |
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| Authors: | Dragovich P S Zhou R Webber S E Prins T J Kwok A K Okano K Fuhrman S A Zalman L S Maldonado F C Brown E L Meador J W Patick A K Ford C E Brothers M A Binford S L Matthews D A Ferre R A Worland S T |
| Affiliation: | Agouron Pharmaceuticals, Inc., San Diego, CA 92121, USA. psd@agouron.com |
| 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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