國家衛生研究院 NHRI:Item 3990099045/1152
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    題名: Design, synthesis, and structure-activity relationships of pyrazolo[3,4-d]pyrimidinies: a novel class of potent enterovirus inhibitors
    其他題名: Design, synthesis, and struc-ture-activity relationships of pyrazolo[3,4-d]pyrimidinies: a novel class of potent enterovirus inhibitors
    作者: Chern, JH;Shia, KS;Hsu, TA;Tai, CL;Lee, CC;Lee, YC;Chang, CS;Tseng, SN;Shih, SR
    貢獻者: Division of Biotechnology and Pharmaceutical Research
    摘要: A series of pyrazolo[3,4-d]pyrimidines were synthesized. and their antiviral activity was evaluated in a plaque reduction assay. It is very interesting that this class of compounds provide remarkable evidence that they are very specific for human enteroviruses, in particular, coxsackieviruses. Some derivatives proved to be highly effective in inhibiting enterovirus replication at nanomolar concentrations. SAR studies revealed that the phenyl group at the N-I position and the hydrophobic diarylmethyl group at the piperazine largely influenced the in vitro antienteroviral activity of this new class of potent antiviral agents. It was found that the pyrazolo[3,4-d]pyrimidines with a thiophene substituent, such as compounds 20 24, in general exhibited high activity against coxsackievirus B3 (IC50 = 0.063-0.089 muM) and moderate activity against enterovirus 71 (IC50 = 0.32-0.65 muM) with no apparent cytotoxic effect toward RD (rhabdomyosarcoma) cell lines (CC50>25 muM). (C) 2004 Elsevier Ltd. All rights reserved.
    關鍵詞: Chemistry, Medicinal;Chemistry, Organic
    日期: 2004-05-17
    關聯: Bioorganic and Medicinal Chemistry Letters. 2004 May;14(10):2519-2525.
    Link to: http://dx.doi.org/10.1016/j.bmcl.2004.02.092
    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:000221316000025
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=1942438497
    顯示於類別:[徐祖安] 期刊論文
    [夏克山] 期刊論文
    [陳志豪] 期刊論文

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