Structure-activity relationship and improved hydrolytic stability of pyrazole derivatives that are allosteric inhibitors of West Nile Virus NS2B-NS3 p...
Basic Information
ID: ALA1156012
Journal: Bioorg Med Chem Lett
Title: Structure-activity relationship and improved hydrolytic stability of pyrazole derivatives that are allosteric inhibitors of West Nile Virus NS2B-NS3 proteinase.
Authors: Sidique S, Shiryaev SA, Ratnikov BI, Herath A, Su Y, Strongin AY, Cosford ND.
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 1-2h. 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.
CiteXplore: 19703770
DOI: 10.1016/j.bmcl.2009.07.150
Patent ID: ┄