Suslov Evgenii V, Mozhaytsev Evgenii S, Korchagina Dina V, Bormotov Nikolay I, Yarovaya Olga I, Volcho Konstantin P, Serova Olga A, Agafonov Alexander P, Maksyutov Rinat A, Shishkina Larisa N, Salakhutdinov Nariman F
Novosibirsk Institute of Organic Chemistry , Siberian Branch of the Russian Academy of Sciences , Lavrentjev Avenue 9 , 630090 Novosibirsk , Russia . Email:
Department of Prevention and Treatment of Especially Dangerous Infections , State Research Center of Virology and Biotechnology VECTOR , Koltsovo , Novosibirsk Region , 630559 , Russian Federation.
RSC Med Chem. 2020 Aug 6;11(10):1185-1195. doi: 10.1039/d0md00108b. eCollection 2020 Oct 1.
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).
目前,针对正痘病毒,尤其是天花病毒的药物种类非常有限。尽管天花已得到有效控制,但由于多种原因,仍存在由该病毒或类似病毒引发疫情的实际威胁。为了寻找新型低分子量正痘病毒抑制剂,以1-金刚烷羧酸和2-金刚烷羧酸以及桃金娘烯酸、香茅酸和樟脑磺酸作为酸组分,合成了一系列结合金刚烷和单萜部分的酰胺。所制备的化合物对痘苗病毒(一种属于痘病毒科的包膜病毒)表现出高活性,且细胞毒性较低。一些化合物的选择性指数高于参考药物西多福韦;含有(-)-10-氨基-2-蒎烯部分的1-金刚烷羧酰胺表现出最高的选择性指数,SI = 1123。所制备的化合物还对其他正痘病毒具有抑制活性:牛痘病毒(SI = 30 - 406)和埃可病毒(鼠痘病毒,SI = 39 - 707)。