期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 24, 期 13, 页码 3035-3042出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.05.013
关键词
MERS-CoV; SARS-Cov; 3CL(pro); Coronavirus; Pyrazolone
资金
- Academia Sinica, Taiwan
Severe acute respiratory syndrome (SARS) led to a life-threatening form of atypical pneumonia in late 2002. Following that, Middle East Respiratory Syndrome (MERS-CoV) has recently emerged, killing about 36% of patients infected globally, mainly in Saudi Arabia and South Korea. Based on a scaffold we reported for inhibiting neuraminidase (NA), we synthesized the analogues and identified compounds with low micromolar inhibitory activity against 3CL(pro) of SARS-CoV and MERS-CoV. Docking studies show that a carboxylate present at either R-1 or R-4 destabilizes the oxyanion hole in the 3CL(pro). Interestingly, 3f, 3g and 3m could inhibit both NA and 3CL(pro) and serve as a starting point to develop broad-spectrum antiviral agents. (C) 2016 Elsevier Ltd. All rights reserved.
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