• Bioorg. Med. Chem. Lett. · Jun 2005

    Comparative Study

    Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.

    • Li-Rung Chen, Yu-Chin Wang, Yi Wen Lin, Shan-Yen Chou, Shyh-Fong Chen, Lee Tai Liu, Ying-Ta Wu, Chih-Jung Kuo, Tom Shieh-Shung Chen, and Shin-Hun Juang.
    • Development Center for Biotechnology, 102, Lane 169, Kang Ning St., Xi Zhi 221, Taipei, Taiwan, ROC.
    • Bioorg. Med. Chem. Lett. 2005 Jun 15; 15 (12): 3058-62.

    AbstractN-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC50 values ranging from 0.95 to 17.50 microM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.

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