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  • 标题:Preparation and Antiviral Activity of Some New C3- and CS-Symmetrical Tri-Substituted Triazine Derivatives Having Benzylamine Substituents
  • 本地全文:下载
  • 作者:Nobuko Mibu ; Kazumi Yokomizo ; Marina Sano
  • 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 CS -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
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