Synthesis and anti-BVDV activity of novel δ-sultones in vitro: Implications for HCV therapies

XuH.-W.; ZhaoL.-J.; LiuH.-F.; ZhaoD.; LuoJ.; XieX.-P.; LiuW.-S.; ZhengJ.-X.; DaiG.-F.; LiuH.-M.; LiuL.-H.; LiangY.-B.

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Synthesis and anti-BVDV activity of novel δ-sultones in vitro: Implications for HCV therapies

机译：新型δ-磺内酯的合成及体外抗BVDV活性：对HCV治疗的意义

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In this study we report the synthesis and activity against bovine viral diarrhea virus (BVDV) of a novel series of bicycle δ-sultones containing γ-lactones. BVDV is responsible for major losses in cattle. Some of the synthesized δ-sultones showed pronounced anti-BVDV activity with EC 50 values of 0.12-1.0 μM and no significant cytotoxicity. Among them, the ortho bromosubstituted derivative 4f (EC50 = 0.12 μM) showed better antiviral activity than other derivatives and was 10 fold more that of than positive control ribavirin (EC50 = 1.3 μM). BVDV is also considered to be a valuable surrogate for the hepatitis C virus (HCV) in antiviral drug studies. The above results provided a novel candidate for the development of anti-HCV agents.

机译：在这项研究中，我们报告了含有γ-内酯的一系列新型自行车δ-内酯的合成及其对牛病毒性腹泻病毒（BVDV）的活性。 BVDV是造成牛群重大损失的原因。一些合成的δ-磺内酯显示出明显的抗BVDV活性，EC 50值为0.12-1.0μM，没有明显的细胞毒性。其中，邻溴取代衍生物4f（EC50 = 0.12μM）显示出比其他衍生物更好的抗病毒活性，是阳性对照利巴韦林（EC50 = 1.3μM）的10倍。在抗病毒药物研究中，BVDV也被认为是丙型肝炎病毒（HCV）的宝贵替代品。以上结果为抗HCV药物的开发提供了新的候选者。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2014年第10期|共4页
作者
XuH.-W.; ZhaoL.-J.; LiuH.-F.; ZhaoD.; LuoJ.; XieX.-P.; LiuW.-S.; ZhengJ.-X.; DaiG.-F.; LiuH.-M.; LiuL.-H.; LiangY.-B.;
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正文语种 eng
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关键词
Anti-BVDV; Anti-HCV; CSIC reaction; Lactone; Sultone; Synthesis;

机译：抗BVDV;抗HCV;CSIC反应;内酯;磺内酯;合成;

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1. Synthesis and anti-BVDV activity of novel δ-sultones in vitro: Implications for HCV therapies [J] . XuH.-W., ZhaoL.-J., LiuH.-F., Bioorganic and Medicinal Chemistry Letters . 2014,第10期

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2. Novel pyrrolo[2,3-d]pyrimidine derivatives: Design, synthesis, structure elucidation and in vitro anti-BVDV activity [J] . Sroor Farid M., Basyouni Wahid M., Tohamy Wael M., Tetrahedron . 2019,第51期

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Synthesis and anti-BVDV activity of novel δ-sultones in vitro: Implications for HCV therapies

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