Patrusheva Oksana S, Zarubaev Vladimir V, Shtro Anna A, Orshanskaya Yana R, Boldyrev Sergey A, Ilyina Irina V, Kurbakova Svetlana Yu, Korchagina Dina V, Volcho Konstantin P, Salakhutdinov Nariman F
Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
Department of Chemotherapy, Influenza Research Institute, 15/17 Prof. Popova St., 197376 St. Petersburg, Russia.
Bioorg Med Chem. 2016 Nov 1;24(21):5158-5161. doi: 10.1016/j.bmc.2016.08.037. Epub 2016 Aug 22.
The antiviral activity of 4-hydroxy-hexahydro-2H-chromenes and 4-fluorine-hexahydro-2H-chromenes with an aromatic substituent, synthesized from monoterpene (-)-verbenone, was studied for the first time. Five of 11 (45 per cent) of 4-hydroxy-hexahydro-2H-chromene-type compounds have been found to exhibit antiviral activity against influenza A virus of subtype H1N1pdm09. Although a portion of active compounds among 4-fluorine-containing series was fewer, just compound 5i that contains a fluorine substituent exhibited more potent anti-influenza activity along with low cytotoxicity. Thus two new promising types of antiviral compounds were identified.
首次研究了由单萜（-）-马鞭草烯酮合成的带有芳香取代基的4-羟基-六氢-2H-色烯和4-氟-六氢-2H-色烯的抗病毒活性。已发现11种4-羟基-六氢-2H-色烯类化合物中的5种（45%）对H1N1pdm09亚型甲型流感病毒具有抗病毒活性。尽管含氟系列中的活性化合物较少，但仅含氟取代基的化合物5i表现出更强的抗流感活性以及低细胞毒性。因此，确定了两种新的有前景的抗病毒化合物类型。
