Anti-influenza activity of monoterpene-containing substituted coumarins
Anti-influenza activity of monoterpene-containing substituted coumarins
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DOI：
10.1016/j.bmcl.2017.04.091
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发表时间：
2017-07-01
影响因子：
2.7
通讯作者：
Salakhutdinov, Nariman F.
中科院分区：
文献类型：
--
作者：
Khomenko, Tatyana M.;Zarubaev, Vladimir V.;Salakhutdinov, Nariman F.
同时携带单萜烯和香豆素部分的化合物已被测试对流感病毒A/California/07/09 (H1N1) pdm09的细胞毒性和抑制活性。香豆素框架中取代基的结构，以及单萜类部分的结构和绝对构型，对所研究化合物的抗流感活性和细胞毒性有显著影响。具有双环蒎烷骨架的化合物表现出最高的选择性指数（细胞毒性与活性剂量之间的比率）。（-）-桃金娘烯醇15c衍生物具有活性好、细胞毒性低、易于合成等特点，在该类化合物中具有较大的应用潜力。在病毒繁殖的早期阶段，将其添加到感染细胞培养物中表现出最高的活性。(C) 2017 Elsevier Ltd.版权所有。
Compounds simultaneously carrying the monoterpene and coumarin moieties have been tested for cytotoxicity and inhibition of activity against influenza virus A/California/07/09 (H1N1) pdm09. The structure of substituents in the coumarin framework, as well as the structure and the absolute configuration of the monoterpenoid moiety, are shown to significantly influence the anti-influenza activity and cytotoxicity of the compounds under study. The compounds with a bicyclic pinane framework exhibit the highest selectivity indices (the ratios between the cytotoxicity and the active dose). The derivative of (-)-myrtenol 15c, which is characterized by promising activity, low cytotoxicity, and synthetic accessibility, has the greatest potential among this group of compounds. It exhibited the highest activity when added to the infected cell culture at early stages of viral reproduction. (C) 2017 Elsevier Ltd. All rights reserved.