2-Amino-6-hydrazino-7H-purine | 5446-90-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 2-Amino-6-hydrazino-7H-purine
• 英文别名: 6-hydrazinyl-7H-purin-2-amine；6-hydrazino-7(9)H-purin-2-ylamine；6-Hydrazino-7(9)H-purin-2-ylamin
• CAS: 5446-90-2
• 化学式: C₅H₇N₇
• mdl: MFCD19203367
• 分子量: 165.157
• InChiKey: KNOLGURLPMQDCC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  119
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-Amino-6-hydrazino-7H-purine 在 盐酸 、 potassium carbonate 作用下， 以 甲醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 26.0h， 生成 9-(2,6-difluorobenzyl)-6-(1H-pyrazol-1-yl)-9H-purin-2-amine
  参考文献：
  名称：

  질소를 포함하는 헤테로고리로 치환된 축합 피리미딘 유도체 및 그의 의약 용도

  摘要：

  这个申请涉及一种含氮杂环取代的嘧啶衍生物及其药用用途，提供了如下化合物，溶剂化合物，立体异构体或其药学上可接受的盐，以及包含它们的用于预防或治疗癌症的药学组合物：[化学式 I]。

  公开号：

  KR20210076693A
• 作为产物：
  描述：

  6-硫鸟嘌呤 在 sodium hydroxide 、 肼 作用下， 反应 2.0h， 生成 2-Amino-6-hydrazino-7H-purine
  参考文献：
  名称：

  Synthesis of Potential Anticancer Agents. III. Hydrazino Analogs of Biologically Active Purines²

  摘要：

  DOI：

  10.1021/ja01566a043

文献信息

• Novel xanthine oxidase inhibitor studies. Part 2. Synthesis and xanthine oxidase inhibitory activities of 2-substituted 6-alkylidenehydrazino- or 6-arylmethylidenehydrazino-7H-purines and 3- and/or 5-substituted 9H-1,2,4-triazolo[3,4-i ]purines
  作者：Tomohisa Nagamatsu、Hiroo Yamasaki、Takayuki Fujita、Kazuki Endo、Haruhiko Machida

  DOI：10.1039/a906230k

  日期：——

  general synthesis of 2-substituted 6-alkylidenehydrazino- or 6-arylmethylidenehydrazino-7H-purines and 3- and/or 5-substituted 9H-1,2,4-triazolo[3,4-i]purines, which were obtained by oxidative cyclisation of the corresponding 6-aldehyde hydrazones of 7H-purine, as a new class of potential xanthine oxidase inhibitors are reported. Their inhibitory activities against bovine milk xanthine oxidase in vitro

  2-取代的6-亚烷基萘并肼基或6-芳基亚甲基肼基并氨基7 H-嘌呤和3-和/或5-取代的9 H -1,2,4-三唑并[3,4- -i ]嘌呤的简便且通用的合成方法，据报道，它们是通过相应的7 H-嘌呤的6-醛的氧化环化而获得的，作为新型潜在的黄嘌呤氧化酶抑制剂。还研究了它们在体外对牛黄嘌呤氧化酶的抑制活性，一些嘌呤2和6和三唑并呋喃酮7的活性比别嘌呤醇高出几倍到几百倍。
• Purine compounds and xanthine oxidase inhibitors
  申请人：Yamasa Corporation

  公开号：US05990118A1

  公开（公告）日：1999-11-23

  Purine or triazolopurine compounds are disclosed represented by formula (I) or (II): ##STR1## wherein R.sup.1 and R.sup.4 represent each hydrogen, halogeno, hydroxy, mercapto, or amino; R.sup.2 represents alkyl or aryl; and R.sup.3 and R.sup.5 represent each hydrogen, alkyl, or aryl; and pharmaceutical compositions comprising these compounds as xanthine oxidase inhibitors, remedies for hyperuricemia, or remedies or preventive agents for gout.

  公开了由公式（I）或（II）表示的嘌呤或三氮杂嘌呤化合物：其中R.sup.1和R.sup.4分别表示氢、卤、羟基、巯基或氨基；R.sup.2表示烷基或芳基；R.sup.3和R.sup.5分别表示氢、烷基或芳基；以及包含这些化合物的药物组合物作为黄嘌呤氧化酶抑制剂、治疗高尿酸血症的药物、或痛风的治疗或预防剂。
• In vitro Antibacterial Evaluation of 1,2,4-Triazole Compounds Containing Purine Moiety
  作者：Sevdije Govori

  DOI：10.1007/s10600-017-2217-7

  日期：2017.11

  9H-[1,2,4]Triazolo[4,3-g]purin-5-amine (2) was synthesized by reaction of 6-hydrazinyl-7H-purin-2-amine (1a) with formic acid under reflux conditions. Treating compound 1a in ethanol with CS2 in the presence of KOH yielded 5-amino-3H-[1,2,4]triazolo[4,3-g]purine-3-thione (3). The new synthesized compounds were characterized using IR, 1H NMR, and elemental analysis. The synthesized compounds have been screened for antibacterial activity.

  在回流条件下，6-肼基-7H-嘌呤-2-胺（1a）与甲酸反应合成了 9H-[1,2,4]三唑并[4,3-g]嘌呤-5-胺（2）。在 KOH 存在下，用 CS2 处理乙醇中的化合物 1a，得到 5-氨基-3H-[1,2,4]三唑并[4,3-g]嘌呤-3-硫酮（3）。利用红外光谱、1H NMR 和元素分析对新合成的化合物进行了表征。对合成的化合物进行了抗菌活性筛选。
• Anti-malarial activity of N6-modified purine analogues
  作者：Kathleen Too、Daniel M. Brown、Emily Bongard、Vanessa Yardley、Livia Vivas、David Loakes

  DOI：10.1016/j.bmc.2007.05.038

  日期：2007.8

  Plasmodium falciparum causes one of the deadliest forms of malaria and resistance to the currently available drugs makes it imperative to develop new, safe and potent drugs. Parasites such as P. falciparum are unable to synthesise purines de novo and to this end often have multiple purine uptake and salvage systems. With this in mind, we have designed and synthesised libraries of purine analogues as potential anti-malarial agents. Herein, we report three compounds with promising activity against the highly chloroquine-resistant VS1 P. falciparum namely: N-6-hydroxyadenine (1c), 2-amino-N-6-aminoadenosine (2b) and 2-amino-N-6-amino-N-6-methyladenosine (4b). (c) 2007 Elsevier Ltd. All rights reserved.