Department of Chemistry & Frontier Research Center on Fundamental and Applied Sciences of Matters, National Tsing Hua University, Hsinchu 30013, Taiwan; Department of Chemistry, National Central University, Jhongli City 32001, Taiwan.
Department of Chemistry & Frontier Research Center on Fundamental and Applied Sciences of Matters, National Tsing Hua University, Hsinchu 30013, Taiwan.
Antiviral Res. 2017 Oct;146:96-101. doi: 10.1016/j.antiviral.2017.08.008. Epub 2017 Aug 19.
There are currently still no approved antiviral drugs to treat or prevent chikungunya virus (CHIKV) infections despite the fact that this arbovirus continues to cause outbreaks in Africa, Asia, and South- and Central-America. Thus 20 new conjugated compounds in the families of bis(benzofuran-1,3-thiazolidin-4-one)s and bis(benzofuran-1,3-thiazinan-4-one)s were designed based on the structural features of suramin. These new compounds were synthesized by chemical methods and their structures were confirmed spectroscopically. In CPE reduction assays, six of these new bis-conjugates inhibited CHIKV replication in Vero E6 cells with EC in the range of 1.9-2.7 μM and selectivity index values of ∼75 or higher. These results and compounds provide a starting point for further optimization, design, and synthesis of new antiviral agents for this (re)emerging disease.
目前，尽管这种虫媒病毒仍继续在非洲、亚洲以及中南美洲引发疫情，但仍没有获得批准的抗病毒药物可用于治疗或预防基孔肯雅病毒（CHIKV）感染。因此，我们基于苏拉明的结构特征，设计了苯并呋喃-1,3-噻唑烷-4-酮和苯并呋喃-1,3-噻唑烷-4-酮两类中的 20 种新的共轭化合物。这些新化合物通过化学方法合成，并通过光谱法确认其结构。在 CPE 还原测定中，这 6 种新的双共轭物对 Vero E6 细胞中的 CHIKV 复制具有抑制作用，EC 值在 1.9-2.7 μM 范围内，选择性指数值约为 75 或更高。这些结果和化合物为针对这种（重新）出现的疾病的新型抗病毒药物的进一步优化、设计和合成提供了起点。
