肽基 α-酮酰胺和 α-酮杂环对诺如病毒 3CL 蛋白酶的强效抑制作用。
Potent inhibition of norovirus 3CL protease by peptidyl α-ketoamides and α-ketoheterocycles.
机构信息
Department of Chemistry, Wichita State University, Wichita, KS 67260, USA.
出版信息
Bioorg Med Chem Lett. 2012 Jul 15;22(14):4820-6. doi: 10.1016/j.bmcl.2012.05.055. Epub 2012 May 26.
Abstract
A series of structurally-diverse α-ketoamides and α-ketoheterocycles was synthesized and subsequently investigated for inhibitory activity against norovirus 3CL protease in vitro, as well as anti-norovirus activity in a cell-based replicon system. The synthesized compounds were found to inhibit norovirus 3CL protease in vitro and to also exhibit potent anti-norovirus activity in a cell-based replicon system.
摘要
合成了一系列结构多样的α-酮酰胺和α-酮杂环化合物，并对其进行了体外抑制诺如病毒 3CL 蛋白酶活性以及基于细胞的复制子系统抗诺如病毒活性的研究。结果表明，所合成的化合物在体外能够抑制诺如病毒 3CL 蛋白酶，并且在基于细胞的复制子系统中具有很强的抗诺如病毒活性。
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