Suppr超能文献

利用点击化学方法合成莰烯衍生物及其抗病毒活性研究。

Synthesis of camphecene derivatives using click chemistry methodology and study of their antiviral activity.

作者信息

Artyushin Oleg I, Sharova Elena V, Vinogradova Natalya M, Genkina Galina K, Moiseeva Aleksandra A, Klemenkova Zinaida S, Orshanskaya Iana R, Shtro Anna A, Kadyrova Renata A, Zarubaev Vladimir V, Yarovaya Olga I, Salakhutdinov Nariman F, Brel Valery K

机构信息

A.N. Nesmeyanov Institute of Organoelement Compounds of Russian Academy of Sciences, 28, Vavilova St., GSP-1, V-334, 119991 Moscow, Russian Federation.

Department of Chemotherapy, Influenza Research Institute, 15/17 Prof. Popova St., 197376 St. Petersburg, Russian Federation.

出版信息

Bioorg Med Chem Lett. 2017 May 15;27(10):2181-2184. doi: 10.1016/j.bmcl.2017.03.051. Epub 2017 Mar 22.

Abstract

A series of seventeen tetrazole derivatives of 1,7,7-trimethyl-[2.2.1]bicycloheptane were synthesized using click chemistry methodology and characterized by spectral data. Studies of cytotoxicity and in vitro antiviral activity against influenza virus A/Puerto Rico/8/34 (H1N1) in MDCK cells of the compounds obtained were performed. The structure-activity relationship analysis suggests that to possess virus-inhibiting activity, the compounds of this group should bear oxygen atom with a short linker (C2-C4), either as a hydroxyl group (18, 19, 29), keto-group (21) or as a part of a heterocycle (24). These compounds demonstrated low cytotoxicity along with high anti-viral activity.

摘要

采用点击化学方法合成了一系列17种1,7,7-三甲基-[2.2.1]双环庚烷的四唑衍生物,并通过光谱数据对其进行了表征。对所获得化合物在MDCK细胞中针对甲型流感病毒A/波多黎各/8/34(H1N1)的细胞毒性和体外抗病毒活性进行了研究。构效关系分析表明,为了具有病毒抑制活性,该类化合物应带有与短连接基(C2 - C4)相连的氧原子,该氧原子可以是羟基(18、19、29)、酮基(21)或作为杂环的一部分(24)。这些化合物表现出低细胞毒性和高抗病毒活性。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验