Inhibition of noroviruses by piperazine derivatives
Inhibition of noroviruses by piperazine derivatives
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DOI：
10.1016/j.bmcl.2011.10.122
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发表时间：
2012-01-01
影响因子：
2.7
通讯作者：
Groutas, William C.
中科院分区：
文献类型：
--
作者：
Dou, Dengfeng;He, Guijia;Groutas, William C.
There is currently an unmet need for the development of small-molecule therapeutics for norovirus infection. The piperazine scaffold, a privileged structure embodied in many pharmacological agents, was used to synthesize an array of structurally-diverse derivatives which were screened for anti-norovius activity in a cell-based replicon system. The studies described herein demonstrate for the first time that functionalized piperazine derivatives possess anti-norovirus activity. Furthermore, these studies have led to the identification of two promising compounds (6a and 9I) that can be used as a launching pad for the optimization of potency, cytotoxicity, and drug-like characteristics. (C) 2011 Elsevier Ltd. All rights reserved.
