Structure–activity relationship and improved hydrolytic stability of pyrazole derivatives that are allosteric inhibitors of West Nile Virus NS2B-NS3 proteinase |
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| Authors: | Shyama Sidique Sergey A Shiryaev Boris I Ratnikov Ananda Herath Ying Su Alex Y Strongin Nicholas DP Cosford |
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| Institution: | 1. Conrad Prebys Center for Chemical Genomics, 10901 N. Torrey Pines Road, La Jolla, CA 92037, USA;2. Burnham Institute for Medical Research, 10901 N. Torrey Pines Road, La Jolla, CA 92037, USA |
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| Abstract: | 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. |
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