(2,4-Diphenylthiazol-5-yl)-(4-pyrrolidin-1-yl-1-piperidyl)methanone | 1314802-64-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (2,4-Diphenylthiazol-5-yl)-(4-pyrrolidin-1-yl-1-piperidyl)methanone
• 英文别名: (2,4-diphenyl-1,3-thiazol-5-yl)-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone
• CAS: 1314802-64-6
• 化学式: C₂₅H₂₇N₃OS
• 分子量: 417.575
• InChiKey: ITGNQXDGWSCKRP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  64.7
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-吡咯烷-1-基哌啶 、 2,4-二苯基-1,3-噻唑-5-羰酰氯 以 二氯甲烷 为溶剂， 反应 3.0h， 生成 (2,4-Diphenylthiazol-5-yl)-(4-pyrrolidin-1-yl-1-piperidyl)methanone
  参考文献：
  名称：

  2,4-Diarylthiazole antiprion compounds as a novel structural class of antimalarial leads

  摘要：

  A significant intersection between antimalarial and antiprion activity is well established for certain compound classes, specifically for polycyclic antimalarial agents bearing basic nitrogen-containing sidechains (e. g., chloroquine, quinacrine, mefloquine). Screening a recently reported set of antiprion compounds with such sidechains showed these 2,4-diarylthiazole based structures also possess significant antimalarial activity. Of particular note, all but one of the compounds displayed activity against a chloroquine-resistant Plasmodium falciparum strain, identifying them as interesting leads for further development in this context. In addition, three new members of the series showed superior antiprion activity compared to the earlier-reported compounds. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.04.090

文献信息

• 2,4-Diarylthiazole antiprion compounds as a novel structural class of antimalarial leads
  作者：Mark J. Thompson、Jennifer C. Louth、Susan M. Little、Beining Chen、Iain Coldham

  DOI：10.1016/j.bmcl.2011.04.090

  日期：2011.6

  A significant intersection between antimalarial and antiprion activity is well established for certain compound classes, specifically for polycyclic antimalarial agents bearing basic nitrogen-containing sidechains (e. g., chloroquine, quinacrine, mefloquine). Screening a recently reported set of antiprion compounds with such sidechains showed these 2,4-diarylthiazole based structures also possess significant antimalarial activity. Of particular note, all but one of the compounds displayed activity against a chloroquine-resistant Plasmodium falciparum strain, identifying them as interesting leads for further development in this context. In addition, three new members of the series showed superior antiprion activity compared to the earlier-reported compounds. (C) 2011 Elsevier Ltd. All rights reserved.