Abstract：
A novel series of benzenesulfonamide substituted spirothiazolidinone derivatives (3a-j) were synthesized, characterized and evaluated for their antiviral activity. The spirocyclic compounds were prepared by the condensation of 4-(aminosulfonyl)-2-methoxybenzohydrazide, appropriate cyclic ketones and 2-mercaptopropionic acid in a one-pot reaction. The structures of the new compounds were established by IR, 1H NMR, 13C NMR (APT), and elemental analysis. The new compounds were evaluated in vitro antiviral activity against influenza A/H1N1, A/H3N2 and B viruses, as well as herpes simplex virus type 1 (HSV-1), respiratory syncytial virus (RSV) and yellow fever virus (YFV). Two derivatives bearing propyl (3d) and tert-butyl (3e) substituents at position 8 of the spiro ring exhibited activity against influenza A/H1N1 virus with EC50 values in the range of 35-45 µM and no cytotoxicity at 100 μM, the highest concentration tested.
摘要：
合成了一系列新型的苯磺酰胺取代的螺噻唑烷酮衍生物（3a-j），表征和评估他们的抗病毒活性。螺环化合物是通过缩合4-（氨基磺酰基）-2-甲氧基苯甲酰肼制备的，适当的环酮和2-巯基丙酸在一锅反应。通过红外光谱确定了新化合物的结构,1HNMR,13CNMR(APT),和元素分析。评价了新化合物对甲型H1N1、甲型H3N2和乙型流感病毒的体外抗病毒活性,以及单纯疱疹病毒1型（HSV-1），呼吸道合胞病毒（RSV）和黄热病病毒（YFV）。在螺环的8位带有丙基（3d）和叔丁基（3e）取代基的两种衍生物对甲型/H1N1流感病毒表现出活性，EC50值在35-45µM范围内，在100μM时无细胞毒性，测试的最高浓度。
