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

Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus.
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Picornavirus,Norovirus和冠状病毒的3C和3C样蛋白酶的大环抑制剂。

DOI:
10.1016/j.bmcl.2013.05.021
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发表时间:
2013-07-01
影响因子:
2.7
通讯作者:
Groutas, William C.
Groutas, William C.
中科院分区:
医学4区
文献类型:
--
作者:
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;Groutas, William C.

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The design, synthesis, and in vitro inhibitory activity of the first series of macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus, are reported. 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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