基于无环磺酰胺骨架的强效诺如病毒抑制剂。
Potent norovirus inhibitors based on the acyclic sulfamide scaffold.
机构信息
Department of Chemistry, Wichita State University, Wichita, KS 67260, USA.
出版信息
Bioorg Med Chem. 2012 Mar 15;20(6):2111-8. doi: 10.1016/j.bmc.2012.01.030. Epub 2012 Feb 2.
Abstract
The development of small molecule therapeutics to combat norovirus infection is of considerable interest from a public health perspective because of the highly contagious nature of noroviruses. A series of amino acid-derived acyclic sulfamide-based norovirus inhibitors has been synthesized and evaluated using a cell-based replicon system. Several compounds were found to display potent anti-norovirus activity, low toxicity, and good aqueous solubility. These compounds are suitable for further optimization of pharmacological and ADMET properties.
摘要
从公共卫生的角度来看，开发小分子治疗药物来对抗诺如病毒感染是非常有意义的，因为诺如病毒具有高度传染性。已经合成了一系列基于氨基酸衍生的无环磺酰胺的诺如病毒抑制剂，并使用基于细胞的复制子系统进行了评估。发现几种化合物具有很强的抗诺如病毒活性、低毒性和良好的水溶性。这些化合物适合进一步优化药理学和 ADMET 性质。
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