文章基本信息

标题：Preparation and Antiviral Activity of Some New C3- and CS-Symmetrical Tri-Substituted Triazine Derivatives Having Benzylamine Substituents
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作者：Nobuko Mibu ; Kazumi Yokomizo ; Marina Sano 等
期刊名称：Chemical and Pharmaceutical Bulletin
印刷版ISSN：0009-2363
电子版ISSN：1347-5223
出版年度：2018
卷号：66
期号：8
页码：830-838
DOI：10.1248/cpb.c18-00274
语种：English
出版社：The Pharmaceutical Society of Japan
摘要：We report the preparation of new C ₃- and C_S -symmetrical molecules constructed on a triazine (TAZ) template. Anti-herpes simplex virus type 1 (anti-HSV-1) and cytotoxic activities against Vero cells of synthesized TAZ derivatives were evaluated. The results suggested that the presence of an electron-donating group(s) on the benzene ring in benzylamine groups on the TAZ template is an important structural factor for expressing a high level of anti-HSV-1 activity and low cytotoxicity for these C ₃ types of TAZ derivatives. Among the tested TAZ derivatives, compounds 4f and 7h showed the highest anti HSV-1 activities (EC₅₀=0.98 and 1.23 µM, respectively) and low cytotoxic activities to Vero cells (50% cytotoxic concentration (CC₅₀)=292.2 and >200 µM, respectively).
关键词：1,3,5-triazine;benzylamine-substituent;C3-symmetry;anti-herpes simplex virus type 1;hydrogen bond donor;structure–activity relationship