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Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors
被引:47
|作者:
Prior, Allan M.
[1
]
Kim, Yunjeong
[2
]
Weerasekara, Sahani
[1
]
Moroze, Meghan
[1
]
Alliston, Kevin R.
[3
]
Uy, Roxanne Adeline Z.
[3
]
Groutas, William C.
[3
]
Chang, Kyeong-Ok
[2
]
Hua, Duy H.
[1
]
机构:
[1] Kansas State Univ, Dept Chem, Manhattan, KS 66506 USA
[2] Kansas State Univ, Coll Vet Med, Dept Diagnost Med & Pathobiol, Manhattan, KS 66506 USA
[3] Wichita State Univ, Dept Chem, Wichita, KS 67260 USA
基金:
美国国家科学基金会;
关键词:
Viral 3C and 3C-like protease inhibitors;
Norovirus;
Human rhinovirus;
Severe acute respiratory syndrome;
coronavirus;
Coronavirus;
229E;
D O I:
10.1016/j.bmcl.2013.09.070
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
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, a-ketoamide, bisulfite adduct, and a-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. (C) 2013 Elsevier Ltd. All rights reserved.
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页码:6317 / 6320
页数:4
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