Macrocyclic Inhibitors of 3C and 3C-like Proteases of Picornavirus, Norovirus, and Coronavirus

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Issue Date
2013-05-16
Authors
Mandadapu, Sivakoteswara Rao
Weerawarna, Pathum M.
Prior, Allan M.
Uy, Roxanne Adeline Z.
Aravapalli, Sridhar
Alliston, Kevin R.
Lushington, Gerald H.
Kim, Yunjeong
Hua, Duy H.
Chang, Kyeong-Ok
Advisor
Citation

Sivakoteswara Rao Mandadapu,Pathum M. Weerawarna,Allan M. Prior, Roxanne Adeline Z. Uy,Sridhar Aravapalli,Kevin R. Alliston,Gerald H. Lushington,Yunjeong Kim,Duy H. Hua,Kyeong-Ok Chang,William C. Groutas. 2013. Macrocyclic Inhibitors of 3C and 3C-like Proteases of Picornavirus, Norovirus, and Coronavirus. -- Bioorganic & Medicinal Chemistry Letters, available May 16, 2013. ISSN 0960-894X, 10.1016/j.bmcl.2013.05.021

Abstract

The design, synthesis, and in vitro evaluation of the first macrocyclic inhibitor of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus are reported. The in vitro inhibitory activity (50% effective concentration) of the macrocyclic inhibitor toward enterovirus 3C protease (CVB3 Nancy strain), and coronavirus (SARS-CoV) and norovirus 3C-like proteases, was determined to be 1.8, 15.5 and 5.1 μM, respectively.

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