Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus

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HuaBioorgMedicinalChemLets2013.pdf (304.25 KB)

Date

Authors

Mandadapu, Sivakoteswara Rao

Weerawarna, Pathum M.

Prior, Allan M.

Uy, Roxanne Adeline Z.

Aravapalli, Sridhar

Alliston, Kevin R.

Lushington, Gerald H.

Chang, Kyeong-Ok

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.

Keywords

Proteases, Picornavirus, Norovirus, Coronavirus, Macrocyclic inhibitors

URI

http://hdl.handle.net/2097/16411

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Chemistry Faculty Research and Publications

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