靛红-β-硫代缩氨基脲类化合物作为有效的单纯疱疹病毒抑制剂。

Isatin-β-thiosemicarbazones as potent herpes simplex virus inhibitors.

机构信息

Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 350, Taiwan, ROC.

出版信息

Bioorg Med Chem Lett. 2011 Apr 1;21(7):1948-52. doi: 10.1016/j.bmcl.2011.02.037. Epub 2011 Feb 15.

DOI:10.1016/j.bmcl.2011.02.037

PMID:21356589

Abstract

A series of isatin-β-thiosemicarbazones have been designed and evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in a plaque reduction assay. Their cytotoxicity was examined using human rhabdomyosarcoma cells (RD cells). Several derivatives of isatin-β-thiosemicarbazone exhibited significant and selective antiviral activity with low cytotoxicity. It was found that the thiourea group at thiosemicarbazone and the NH functionality at isatin were essential for their antiherpetic activity. The synthesis and structure-activity relationship studies are presented.

摘要

设计并评估了一系列色酮-β-缩氨基硫脲，以在蚀斑减少测定法中针对单纯疱疹病毒 1 型（HSV-1）和 2 型（HSV-2）进行抗病毒活性。使用人横纹肌肉瘤细胞（RD 细胞）检查它们的细胞毒性。几种色酮-β-缩氨基硫脲衍生物具有显著且选择性的抗病毒活性，同时细胞毒性低。发现缩氨基硫脲基团和色酮上的 NH 官能团对于其抗疱疹活性是必不可少的。介绍了它们的合成和构效关系研究。