Sokolova Anastasiya S, Yarovaya Olga I, Bormotov Nikolay I, Shishkina Larisa N, Salakhutdinov Nariman F
Novosibirsk Institute of Organic Chemistry , Siberian Branch of the Russian Academy of Sciences , Lavrentjev Avenue 9 , 630090 Novosibirsk , Russia . Email:
Novosibirsk State University , Pirogova St. 2 , 630090 Novosibirsk , Russia.
Medchemcomm. 2018 Sep 19;9(10):1746-1753. doi: 10.1039/c8md00347e. eCollection 2018 Oct 1.
The genus belongs to the Poxviridae family and includes variola virus (smallpox), cowpox virus, monkeypox virus and vaccinia virus (VV). Smallpox is considered one of the great epidemic disease scourges in human history. It has currently been eradicated; however, it remains a considerable threat as a biowarfare or bioterrorist weapon. The poxvirus, VV, serves as a model virus from which new antiviral therapies against can be identified. Here, a series of nitrogen-sulphur containing heterocycles such as 1,3-thiazolidin-4-one and thiazoles containing a 1,7,7-trimethylbicyclo[2.2.1]heptan scaffold were synthesized and screened for their antiviral activity. The bioassay results showed that the , and thiazoles, which contained a substituted benzene ring, were able to inhibit VV reproduction with IC values in the 2.4-3.7 micromolar range whilst exhibiting moderate cytotoxicity. Among the thiazolidin-4-one derivatives, compound , which contained a 4-methylbenzylidene group, displayed good inhibitory activity (IC = 9.5 μM) and moderate toxicity.
该属属于痘病毒科，包括天花病毒（天花）、牛痘病毒、猴痘病毒和痘苗病毒（VV）。天花被认为是人类历史上最严重的流行病灾难之一。目前天花已被根除；然而，作为生物战或生物恐怖武器，它仍然构成相当大的威胁。痘苗病毒作为一种模型病毒，可从中鉴定出新型抗病毒疗法。在此，合成了一系列含氮硫杂环化合物，如1,3-噻唑烷-4-酮和含有1,7,7-三甲基双环[2.2.1]庚烷骨架的噻唑，并对其抗病毒活性进行了筛选。生物测定结果表明，含有取代苯环的噻唑、噻唑和噻唑能够抑制痘苗病毒的繁殖，IC值在2.4-3.7微摩尔范围内，同时表现出中等细胞毒性。在噻唑烷-4-酮衍生物中，含有4-甲基亚苄基的化合物表现出良好的抑制活性（IC = 9.5 μM）和中等毒性。
