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2-取代苯并恶嗪酮类似物作为抗人冠状病毒（抗-HCoV）和细胞间黏附分子-1（ICAM-1）表达抑制剂。

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

作者信息

Hsieh Pei-Wen, Chang Fang-Rong, Chang Cheng-Hsien, Cheng Pei-Wen, Chiang Lien-Chai, Zeng Fu-Long, Lin Kuei-Hsiang, Wu Yang-Chang

机构信息

Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan.

出版信息

Bioorg Med Chem Lett. 2004 Sep 20;14(18):4751-4. doi: 10.1016/j.bmcl.2004.06.083.

DOI:10.1016/j.bmcl.2004.06.083
PMID:15324901
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7126427/
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.

摘要

合成了一系列2-取代苯并恶嗪酮，并进行了抗人冠状病毒和ICAM-1表达抑制试验。其中，化合物1、3、4、5、6和7表现出显著的抗HCoV活性，这些化合物的IC(50)值分别为6.08、5.06、6.83、1.92、7.59和5.79μg/mL。此外，化合物1和6对ICAM-1表达显示出显著的抑制作用，1和6的ED(50)值分别为1.00和0.50μg/mL。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3fcc/7126427/b5605450bdcf/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3fcc/7126427/c721c64964e3/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3fcc/7126427/02f330822a7d/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3fcc/7126427/b5605450bdcf/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3fcc/7126427/c721c64964e3/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3fcc/7126427/02f330822a7d/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3fcc/7126427/b5605450bdcf/gr2.jpg

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