期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 19, 页码 5773-5777出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.150
关键词
West Nile virus; Flavivirus; Proteinase inhibitors; NS2B-NS3 proteinase; Antiviral
资金
- NIH [U01 AI078048, U54 HG005033]
West Nile Virus (WNV) is a potentially deadly mosquito-borne flavivirus which has spread rapidly throughout the world. Currently there is no effective vaccine against flaviviral infections. We previously reported the identification of pyrazole ester derivatives as allosteric inhibitors of WNV NS2B-NS3 proteinase. These compounds degrade rapidly in pH 8 buffer with a half life of 1-2 h. We now report the design, synthesis and in vitro evaluation of pyrazole derivatives that are inhibitors of WNV NS2B-NS3 proteinase with greatly improved stability in the assay medium. (C) 2009 Elsevier Ltd. All rights reserved.
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