2-substituted benzoxazinone analogues as anti-human coronavirus (anti-HCoV) and ICAM-1 expression inhibition agents

被引:58
作者
Hsieh, PW
Chang, FR
Chang, CH
Cheng, PW
Chiang, LC
Zeng, FL
Lin, KH
Wu, YC [1 ]
机构
[1] Kaohsiung Med Univ, Grad Inst Nat Products, Kaohsiung 807, Taiwan
[2] Kaohsiung Med Univ, Dept Ophthalmol, Kaohsiung, Taiwan
[3] Kaohsiung Med Univ, Dept Microbiol, Kaohsiung 807, Taiwan
[4] Kaohsiung Med Univ, Dept Lab Diagnosis, Virol Lab, Kaohsiung 807, Taiwan
关键词
benzoxazinones; Anti-HCoVs; ICAM-1;
D O I
10.1016/j.bmcl.2004.06.083
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
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 IC50 value of these compounds are 6.08, 5.06, 6.83, 1.92, 7.59, and 5.79 mug/mL, respectively. Furthermore, compounds 1 and 6 showed significant inhibitory effect on ICAM-1 expression, the ED50 values of 1 and 6 are 1.00 and 0.50 mug/mL, respectively. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4751 / 4754
页数:4
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