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New chemical agents based on adamantane–monoterpene conjugates against orthopoxvirus infections
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-08-06 , DOI: 10.1039/d0md00108b Evgenii V Suslov 1 , Evgenii S Mozhaytsev 1 , Dina V Korchagina 1 , Nikolay I Bormotov 2 , Olga I Yarovaya 1, 3 , Konstantin P Volcho 1, 3 , Olga A Serova 2 , Alexander P Agafonov 2 , Rinat A Maksyutov 2 , Larisa N Shishkina 2 , Nariman F Salakhutdinov 1, 3
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-08-06 , DOI: 10.1039/d0md00108b Evgenii V Suslov 1 , Evgenii S Mozhaytsev 1 , Dina V Korchagina 1 , Nikolay I Bormotov 2 , Olga I Yarovaya 1, 3 , Konstantin P Volcho 1, 3 , Olga A Serova 2 , Alexander P Agafonov 2 , Rinat A Maksyutov 2 , Larisa N Shishkina 2 , Nariman F Salakhutdinov 1, 3
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Currently, the spectrum of agents against orthopoxviruses, in particular smallpox, is very narrow. Despite the fact that smallpox is well controlled, there is, for many reasons, a real threat of epidemics associated with this or a similar virus. In order to search for new low molecular weight orthopoxvirus inhibitors, a series of amides combining adamantane and monoterpene moieties were synthesized using 1- and 2-adamantanecarboxylic acids as well as myrtenic, citronellic and camphorsulfonic acids as acid components. The produced compounds exhibited high activity against the vaccinia virus (an enveloped virus belonging to the poxvirus family), which was combined with low cytotoxicity. Some compounds had a selectivity index higher than that of the reference drug cidofovir; the highest SI = 1123 was exhibited by 1-adamantanecarboxylic acid amide containing the (−)-10-amino-2-pinene moiety. The produced compounds demonstrated inhibitory activity against other orthopoxviruses: cowpox virus (SI = 30–406) and ectromelia virus (mousepox virus, SI = 39–707).
中文翻译：
基于金刚烷-单萜缀合物的抗正痘病毒感染的新型化学制剂
目前，针对正痘病毒、特别是天花的药物谱非常狭窄。尽管天花得到了很好的控制，但由于多种原因，与这种病毒或类似病毒相关的流行病确实存在威胁。为了寻找新的低分子量正痘病毒抑制剂，以1-和2-金刚烷甲酸以及肉豆蔻酸、香茅酸和樟脑磺酸为酸组分，合成了一系列结合金刚烷和单萜部分的酰胺。所产生的化合物对痘苗病毒（属于痘病毒家族的一种有包膜病毒）表现出高活性，同时具有低细胞毒性。部分化合物的选择性指数高于对照药西多福韦；含有(−)-10-氨基-2-蒎烯部分的1-金刚烷甲酰胺表现出最高的SI = 1123。产生的化合物对其他正痘病毒具有抑制活性：牛痘病毒（SI = 30-406）和鼠痘病毒（鼠痘病毒，SI = 39-707）。
更新日期：2020-08-06
中文翻译：
基于金刚烷-单萜缀合物的抗正痘病毒感染的新型化学制剂
目前，针对正痘病毒、特别是天花的药物谱非常狭窄。尽管天花得到了很好的控制，但由于多种原因，与这种病毒或类似病毒相关的流行病确实存在威胁。为了寻找新的低分子量正痘病毒抑制剂，以1-和2-金刚烷甲酸以及肉豆蔻酸、香茅酸和樟脑磺酸为酸组分，合成了一系列结合金刚烷和单萜部分的酰胺。所产生的化合物对痘苗病毒（属于痘病毒家族的一种有包膜病毒）表现出高活性，同时具有低细胞毒性。部分化合物的选择性指数高于对照药西多福韦；含有(−)-10-氨基-2-蒎烯部分的1-金刚烷甲酰胺表现出最高的SI = 1123。产生的化合物对其他正痘病毒具有抑制活性：牛痘病毒（SI = 30-406）和鼠痘病毒（鼠痘病毒，SI = 39-707）。
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