國家衛生研究院 NHRI:Item 3990099045/1134
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    题名: Synthesis and antienteroviral activity of a series of novel, oxime ether-containing pyridyl imidazolidinones
    作者: Chern, JH;Lee, CC;Chang, CS;Lee, YC;Tai, CL;Lin, YT;Shia, KS;Lee, CY;Shih, SR
    贡献者: Division of Biotechnology and Pharmaceutical Research
    摘要: A series of novel, oxime ether-containing pyridyl imidazolidinones were synthesized and their antiviral activity was evaluated in a plaque reduction assay. It is very interesting that this class of compounds is specific for human enteroviruses, in particular, enterovirus 71 (EV71). Some derivatives strongly inhibited enterovirus replication with activities higher or comparable to those of the reference compounds such as A(1) and A(2). Preliminary SAR studies revealed that the chain length of the alkyl linker and the alkyl substituent at the oxime ether group largely influenced the in vitro anti-EV71 activity of this new class of potent antiviral agents. Among this series of compounds synthesized, the pyridyl imidazolidinone with an ethyl oxime ether group located at the para position of the phenoxyl ring (8b) was identified as the most potent enterovirus 71 inhibitor (IC50 = 0-001 muM) with no apparent cytotoxic effect toward RD (rhabdomyosarcoma) cell lines (CC50 > 25 muM). Furthermore, this compound has been shown broad-spectrum activity against most of the serotypes of enteroviruses tested in the nanomolar range. (C) 2004 Elsevier Ltd. All rights reserved.
    关键词: Chemistry, Medicinal;Chemistry, Organic
    日期: 2004-10-18
    關聯: Bioorganic and Medicinal Chemistry Letters. 2004 Oct;14(20):5051-5056.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2004.07.084
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0960-894X&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000224165900005
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=4544319944
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