Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Massarenti 9, 40138 Bologna, Italy.
Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
Molecules. 2019 Mar 15;24(6):1037. doi: 10.3390/molecules24061037.
Parvovirus B19 (B19V) is a human pathogenic virus associated with a wide range of clinical conditions. Currently, there are no recognized antiviral drugs for B19V treatment; therefore, efforts in the search for compounds inhibiting B19V replication are now being pursued. Coumarins (chromen-2-ones) are considered a privileged structure for designing novel orally bioavailable and non-peptidic antiviral agents. To further contribute to the development of new drugs against B19V, our research was focused on the synthesis, characterization and evaluation of antiviral activity of some new 3-(imidazo[2,1-]thiazol-6-yl)-2H-chromen-2-one derivatives. The effects of the synthesized compounds on cell viability and viral replication were investigated by employing two relevant cellular systems, the myeloblastoid cell line UT7/EpoS1 and primary erythroid progenitor cells (EPCs). Some of the tested compounds showed inhibitory activity both on cell viability and on viral replication, depending on the cellular system. These results suggest that the mechanism involved in biological activity is sensitive to small structural changes and that it is possible to direct the activity of the 3-(imidazo[2,1-]thiazol-6-yl)-2H-chromen-2-one core.
细小病毒 B19（B19V）是一种与多种临床病症相关的人类致病病毒。目前，尚无针对 B19V 的公认抗病毒药物；因此，现在正在努力寻找抑制 B19V 复制的化合物。香豆素（色烯-2-酮）被认为是设计新型口服生物利用度和非肽类抗病毒药物的优势结构。为了进一步为针对 B19V 的新药研发做出贡献，我们的研究集中在一些新型 3-（咪唑并[2,1-b]噻唑-6-基）-2H-色烯-2-酮衍生物的合成、表征和抗病毒活性评价上。通过使用两个相关的细胞系统，髓样白血病细胞系 UT7/EpoS1 和原代红细胞祖细胞（EPC），研究了合成化合物对细胞活力和病毒复制的影响。一些测试的化合物对细胞活力和病毒复制都具有抑制活性，这取决于细胞系统。这些结果表明，参与生物活性的机制对微小的结构变化敏感，并且可以对 3-（咪唑并[2,1-b]噻唑-6-基）-2H-色烯-2-酮核心的活性进行定向。
