O. V. Andreeva, M. M. Shulaeva, L. F. Saifina, B. F. Garifullin, M. G. Belenok, V. V. Zarubaev, A. V. Slita, V. E. Semenov, V. E. Kataev
{"title":"1,2,3-三唑基核苷类似物同二聚体的合成和抗病毒活性","authors":"O. V. Andreeva, M. M. Shulaeva, L. F. Saifina, B. F. Garifullin, M. G. Belenok, V. V. Zarubaev, A. V. Slita, V. E. Semenov, V. E. Kataev","doi":"10.1007/s11172-024-4296-5","DOIUrl":null,"url":null,"abstract":"<div><p>New homodimers of 1,2,3-triazolyl nucleoside analogs based on 6-methyluracil, which are linked by the polymethylene linker at the N(1) or N(3) atoms, were synthesized. Screening of <i>in vitro</i> antiviral activity against influenza A virus (H1N1) and Coxsackievirus B3 revealed the lead compound that <i>in vitro</i> inhibited the replication of Coxsackievirus B3 with a half-maximal inhibitory concentration (IC<sub>50</sub>) and a half-maximal cytotoxic concentration (CC<sub>50</sub>) of 30.1 and >374 µmol L<sup>−1</sup>, respectively. A dependence of the antiviral activity on the length of the polymethylene linker connecting the 6-methyluracil and 1,2,3-triazolyl-β-<span>d</span>-ribofuranosyl fragments was found.</p></div>","PeriodicalId":756,"journal":{"name":"Russian Chemical Bulletin","volume":"73 6","pages":"1789 - 1800"},"PeriodicalIF":1.7000,"publicationDate":"2024-07-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and antiviral activity of homodimers of 1,2,3-triazolyl nucleoside analogs\",\"authors\":\"O. V. Andreeva, M. M. Shulaeva, L. F. Saifina, B. F. Garifullin, M. G. Belenok, V. V. Zarubaev, A. V. Slita, V. E. Semenov, V. E. Kataev\",\"doi\":\"10.1007/s11172-024-4296-5\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>New homodimers of 1,2,3-triazolyl nucleoside analogs based on 6-methyluracil, which are linked by the polymethylene linker at the N(1) or N(3) atoms, were synthesized. Screening of <i>in vitro</i> antiviral activity against influenza A virus (H1N1) and Coxsackievirus B3 revealed the lead compound that <i>in vitro</i> inhibited the replication of Coxsackievirus B3 with a half-maximal inhibitory concentration (IC<sub>50</sub>) and a half-maximal cytotoxic concentration (CC<sub>50</sub>) of 30.1 and >374 µmol L<sup>−1</sup>, respectively. A dependence of the antiviral activity on the length of the polymethylene linker connecting the 6-methyluracil and 1,2,3-triazolyl-β-<span>d</span>-ribofuranosyl fragments was found.</p></div>\",\"PeriodicalId\":756,\"journal\":{\"name\":\"Russian Chemical Bulletin\",\"volume\":\"73 6\",\"pages\":\"1789 - 1800\"},\"PeriodicalIF\":1.7000,\"publicationDate\":\"2024-07-26\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Russian Chemical Bulletin\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s11172-024-4296-5\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Russian Chemical Bulletin","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1007/s11172-024-4296-5","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Synthesis and antiviral activity of homodimers of 1,2,3-triazolyl nucleoside analogs
New homodimers of 1,2,3-triazolyl nucleoside analogs based on 6-methyluracil, which are linked by the polymethylene linker at the N(1) or N(3) atoms, were synthesized. Screening of in vitro antiviral activity against influenza A virus (H1N1) and Coxsackievirus B3 revealed the lead compound that in vitro inhibited the replication of Coxsackievirus B3 with a half-maximal inhibitory concentration (IC50) and a half-maximal cytotoxic concentration (CC50) of 30.1 and >374 µmol L−1, respectively. A dependence of the antiviral activity on the length of the polymethylene linker connecting the 6-methyluracil and 1,2,3-triazolyl-β-d-ribofuranosyl fragments was found.
期刊介绍：
Publishing nearly 500 original articles a year, by leading Scientists from Russia and throughout the world, Russian Chemical Bulletin is a prominent international journal. The coverage of the journal spans practically all areas of fundamental chemical research and is presented in five sections:
General and Inorganic Chemistry;
Physical Chemistry;
Organic Chemistry;
Organometallic Chemistry;
Chemistry of Natural Compounds and Bioorganic Chemistry.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
