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2-Substituted benzoxazinone analogues as anti-human coronavirus (anti-HCoV) and ICAM-1 expression inhibition agents
Authors:Hsieh Pei-Wen  Chang Fang-Rong  Chang Cheng-Hsien  Cheng Pei-Wen  Chiang Lien-Chai  Zeng Fu-Long  Lin Kuei-Hsiang  Wu Yang-Chang
Affiliation:Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
Abstract:A series of 2-substituted benzoxazinones were synthesized and subjected to anti-human coronavirus and ICAM-1 expression inhibition assays. Among them, compounds 1, 3, 4, 5, 6, and 7 exhibited significant anti-HCoV activities, and the IC(50) value of these compounds are 6.08, 5.06, 6.83, 1.92, 7.59, and 5.79 microg/mL, respectively. Furthermore, compounds 1 and 6 showed significant inhibitory effect on ICAM-1 expression, the ED(50) values of 1 and 6 are 1.00 and 0.50 microg/mL, respectively.
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