...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Archiv der Pharmazie >Design, Synthesis, and the Biological Evaluation of a New Series of Acyclic 1,2,3-Triazole Nucleosides
【24h】

Design, Synthesis, and the Biological Evaluation of a New Series of Acyclic 1,2,3-Triazole Nucleosides

机译：设计，合成和新系列共循环1,2,3-三唑核苷的生物学评价

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

A new strategy for the synthesis of N-3-benzoylated- and N-3-benzylated N-1-propargylquinazoline-2,4-diones 30a-d and 31a-d from isatoic anhydride 41 is reported. The alkynes 30a-d and 31a-d were applied in the 1,3-dipolar cycloadditions with azides 27 and 28 to synthesize acyclic 1,2,3-triazole nucleosides. The obtained alkynes and 1,2,3-triazole were evaluated for antiviral activity against a broad range of DNA and RNA viruses. The alkyne 30d showed activity against adenovirus-2 (EC50=8.3M), while compounds 37a and 37d were also active toward herpes simplex virus-1 wild-type and thymidine kinase deficient (HSV-1 TK-) strains (EC50 values in the range of 4.6-13.8M). In addition, compounds 30a, 30b, 37b, and 37c exhibited activity toward varicella-zoster virus (VZV) TK+ and TK- strains (EC50=2.1-9.5M). The compound 30b proved to be the most selective against VZV and displayed marginal activity against human cytomegalovirus (HCMV). Although the compound 30a had improved anti-HCMV activity, the increase in anti-HCMV activity was accompanied by significant toxicity. Compounds 37a and 37d showed inhibitory effects toward the human T lymphocyte (CEM) cell line (IC50=21 +/- 7 and 22 +/- 1M, respectively), while compound 35 exhibited cytostatic activity toward HMEC-1 cells (IC50=28 +/- 2 mu M).
机译：据报道了一种新的N-3-苯甲酰化 - 和N-3-苄基化的N-1-丙基喹啉-2,4-二硫代硫醚30A-D和31A-D的新策略。将炔烃30A-D和31A-D施用于含叠氮化物27和28的1,3-偶极环加法中，以合成共循环1,2,3-三唑核苷。评估所得alkynes和1,2,3-三唑针对广泛的DNA和RNA病毒进行抗病毒活性。炔烃30D向腺病毒-2（EC50 = 8.3M）显示出活性，而化合物37A和37D也朝向单纯疱疹病毒-1野生型和胸苷激酶缺陷（HSV-1 TK-）菌株（EC50值范围为4.6-13.8m）。此外，化合物30A，30B，37B和37C表现出朝鲜菌氏菌 - 带状疱疹病毒（VZV）TK +和TK-菌株的活性（EC50 = 2.1-9.5M）。化合物30B被证明是对VZV最有选择的，并针对人巨细胞病毒（HCMV）显示边缘活动。虽然化合物30A具有改善的抗HCMV活性，但抗HCMV活性的增加伴随着显着的毒性。化合物37a和37d显示对人T淋巴细胞（CEM）细胞系（分别分别的抑制作用（分别为21 +/- 7和22 +/-1m），而化合物35向HMEC-1细胞表现出细胞抑制活性（IC50 = 28 +/- 2 mu m）。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号