期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 12, 页码 2165-2170出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.05.012
关键词
Norovirus; Antiviral; Protease inhibitor; Peptide
资金
- NIH [5P30-AI-50409]
- Wayne State University
A series of tripeptidyl transition state inhibitors with new PI and warhead moieties were synthesized and evaluated in a GI-1 norovirus replicon system and against GII-4 and GI-1 norovirus proteases. Compound 19, containing a 6-membered ring at the P1 position and a reactive aldehyde warhead exhibited submicromolar replicon inhibition. Retaining the same peptidyl scaffold, several reactive warheads were tested for protease inhibition and norovirus replicon inhibition. Of the six that were synthesized and tested, compounds 42,43, and 45 potently inhibited the protease in biochemical assay and GI-1 norovirus replicon in the nanomolar range.
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