8-nitrophthalazine-5-amine | 502584-69-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 8-nitrophthalazine-5-amine
• 英文别名: 5-nitro-8-aminophthalazine；8-Nitrophthalazin-5-amine；8-nitrophthalazin-5-amine
• CAS: 502584-69-2
• 化学式: C₈H₆N₄O₂
• 分子量: 190.161
• InChiKey: PEUAMCAQIPGEKL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  97.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  8-nitrophthalazine-5-amine 在 palladium on activated charcoal 盐酸 、 sodium chlorate 、 氢气 作用下， 以 乙醇 为溶剂， 20.0~65.0 ℃ 、20.68 kPa 条件下， 反应 3.0h， 生成 6,7-二氯酞嗪-5,8-二酮
  参考文献：
  名称：

  Synthesis and antifungal activity of 6-arylamino-phthalazine-5,8-diones and 6,7-bis(arylthio)-phthalazine-5,8-diones

  摘要：

  6-Arylamino-phthalazine-5,8-diones and 6,7-bis(arylthio)-phthalazine-5,8-diones were synthesized and tested for in vitro antifungal activity against two pathogenic strains of fungi. Among those tested, many compounds showed good antifungal activity. The results suggest that phthalazine-5,8-diones would be potent antifungal agents. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.02.003
• 作为产物：
  描述：

  5-硝基酞嗪 在 盐酸羟胺 、 sodium hydroxide 作用下， 以 乙醇 为溶剂， 生成 8-nitrophthalazine-5-amine
  参考文献：
  名称：

  Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors

  摘要：

  A series of novel indolizinophthalazine-5,12-dione derivatives were designed and synthesized by the reaction of 6,7-dichlorophthalazine-5,8-dione with active methylene reagents (AMR) and pyridine derivatives. Some of synthesized compounds exhibited significant in vitro antiproliferative activity at micromolar level toward four human tumor cell lines, including lung adenocarcinoma cell, large-cell lung carcinoma cell, breast carcinoma cell and ardriamycin-resistance breast carcinoma cell. The DNA topoisomerase IB inhibitory assay indicated that DNA topoisomerase IB might be a biological target of the synthesized compounds. (C) 2010 Published by Elsevier Masson SAS.

  DOI：

  10.1016/j.ejmech.2010.05.048

文献信息

• Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors
  作者：De-Qing Shen、Zu-Ping Wu、Xi-Wei Wu、Zeng-Yun An、Xiang-Zhang Bu、Lian-Quan Gu、Zhi-Shu Huang、Lin-Kun An

  DOI：10.1016/j.ejmech.2010.05.048

  日期：2010.9

  A series of novel indolizinophthalazine-5,12-dione derivatives were designed and synthesized by the reaction of 6,7-dichlorophthalazine-5,8-dione with active methylene reagents (AMR) and pyridine derivatives. Some of synthesized compounds exhibited significant in vitro antiproliferative activity at micromolar level toward four human tumor cell lines, including lung adenocarcinoma cell, large-cell lung carcinoma cell, breast carcinoma cell and ardriamycin-resistance breast carcinoma cell. The DNA topoisomerase IB inhibitory assay indicated that DNA topoisomerase IB might be a biological target of the synthesized compounds. (C) 2010 Published by Elsevier Masson SAS.
• Synthesis and antifungal activity of 6-arylamino-phthalazine-5,8-diones and 6,7-bis(arylthio)-phthalazine-5,8-diones
  作者：Chung-Kyu Ryu、Rae-Eun Park、Mi-Young Ma、Ji-Hee Nho

  DOI：10.1016/j.bmcl.2007.02.003

  日期：2007.5

  6-Arylamino-phthalazine-5,8-diones and 6,7-bis(arylthio)-phthalazine-5,8-diones were synthesized and tested for in vitro antifungal activity against two pathogenic strains of fungi. Among those tested, many compounds showed good antifungal activity. The results suggest that phthalazine-5,8-diones would be potent antifungal agents. (c) 2007 Elsevier Ltd. All rights reserved.