Bulletin of the Korean chemical society | |
Synthesis and Evaluation of Benzoquinolinone Derivatives as SARS-CoV 3CL Protease Inhibitors | |
Young Sik Jung1  Deok Chan Ha1  Chih Jung Kuo1  Hun Ge Liu1  Po Huang Liang1  Tae Young Ahn1  | |
关键词: Benzoquinoline; Coronavirus; Picornavirus; 3C protease; Computer modeling; | |
DOI : | |
学科分类:化学(综合) | |
来源: Korean Chemical Society | |
【 摘 要 】
For the discovery of new antivirals against Severe Acute Respiratory Syndrome-coronavirus (SARS-CoV), we prepared and evaluated several benzoquinoline compounds as its 3C-like protease (3CLpro) inhibitors. Based on the computer modeling study that each of the two rigid benzoquinolinone and N-phenoltetrazole moieties of the compound 1 is bound to the S1 and S2 sites, respectively, of the SARS protease by forming H-bonds and hydrophobic interactions, we designed and synthesized alkylated benzoquinolines at both the sites of the hydroxyl groups. We found that the compound 2a showed five times higher inhibiting activity against the 3CLpro compared to the compound 1.
【 授权许可】
Unknown
【 预 览 】
Files | Size | Format | View |
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RO201912010241804ZK.pdf | 420KB | download |