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Title: Design, synthesis and biological evaluation of inhibitors of flavivirus NS2B/NS3 protease
Keywords: Flavivirus, NS2B/NS3 Protease, Inhibitor, Cyclopeptide, Small molecule
Issue Date: 4-Aug-2009
Citation: GAO YAOJUN (2009-08-04). Design, synthesis and biological evaluation of inhibitors of flavivirus NS2B/NS3 protease. ScholarBank@NUS Repository.
Abstract: Dengue and West Nile virus which belong to the flavivirus family cause severe and often fatal diseases in humans and animals. Currently, there are no approved vaccines or antiviral therapeutics available. These viruses encode a NS2B/NS3 serine protease that is essential for viral replication cycle was identified as an excellent therapeutic target. This thesis mainly focuses on finding potential inhibitors of the Den and WNV NS2B/NS3 proteases. For the dengue NS2B/NS3 protease, a new approach to obtain cyclotide analogues based on the bacterial expression was designed. Two fully oxidized forms of a cyclotide analogue were found showing potent inhibition with Ki of 1.39B1 0.35 and 3.03 B11 0.75 N<M, respectively. For the WNV NS2B/NS3 protease, a potent, stable molecule with Ki value of 1.82B10.58 N<M was identified to be an uncompetitive inhibitor. In addition, this thesis comprises a methodology development part of solid-phase synthesis of pyrazolo[5,1-d][1,2,3,5] tetrazine-4(3H)-ones. A one-pot reaction from 5-aminopyrazoles to the pyrazolo[5,1-d][1,2,3,5] tetrazine-4(3H)-ones provided 16 compounds in good yields.
Appears in Collections:Ph.D Theses (Open)

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