Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors.

Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors.
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DOI:
10.1016/j.bmcl.2013.09.070
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发表时间:
2013-12-01
影响因子:
2.7
通讯作者:
Hua, Duy H.
Hua, Duy H.
中科院分区:
医学4区
文献类型:
--
作者:
Prior, Allan M.;Kim, Yunjeong;Weerasekara, Sahani;Moroze, Meghan;Alliston, Kevin R.;Uy, Roxanne Adeline Z.;Groutas, William C.;Chang, Kyeong-Ok;Hua, Duy H.

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A class of tripeptidyl transition state inhibitors containing a P1 glutamine surrogate, a P2 leucine, and a P3 arylalanines, was found to potently inhibit Norwalk virus replication in enzyme and cell based assays. An array of warheads, including aldehyde, α-ketoamide, bisulfite adduct, and α-hydroxyphosphonate transition state mimic, was also investigated. Tripeptidyls 2 and 6 possess antiviral activities against noroviruses, human rhinovirus, severe acute respiratory syndrome coronavirus, and coronavirus 229E, suggesting a broad range of antiviral activities.
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