• Bioorg. Med. Chem. · Jul 2016

    Identification, synthesis and evaluation of SARS-CoV and MERS-CoV 3C-like protease inhibitors.

    • Vathan Kumar, Kian-Pin Tan, Ying-Ming Wang, Sheng-Wei Lin, and Po-Huang Liang.
    • Institute of Biological Chemistry, Academia Sinica, Taipei 115, Taiwan.
    • Bioorg. Med. Chem. 2016 Jul 1; 24 (13): 3035-3042.

    AbstractSevere 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.Copyright © 2016 Elsevier Ltd. All rights reserved.

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