3-氨基苯-1,2-二甲酸二酰肼 | 16031-26-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 3-氨基苯-1,2-二甲酸二酰肼
• 英文名称: Luminol
• 英文别名: 3-Aminobenzene-1,2-dicarbohydrazide
• CAS: 16031-26-8
• 化学式: C₈H₁₁N₅O₂
• 分子量: 209.208
• InChiKey: UMULKNIDVSBBLE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  136
• 氢给体数：
  5
• 氢受体数：
  5

安全信息

• 海关编码：
  2928000090

反应信息

• 作为反应物：
  描述：

  3-氨基苯-1,2-二甲酸二酰肼 、 马来酸酐 在 乙醚 作用下， 以 溶剂黄146 为溶剂， 反应 2.0h， 以2.15 grams of luminol-maleamic acid was obtained的产率得到Luminol maleamic acid
  参考文献：
  名称：

  Isomaleimide and isophthalamide derivatives of chromophors

  摘要：

  提供了一种具有色团化合物的新异马来酰亚胺和异苯二甲酰亚胺衍生物，可用于分析技术，用于检测和测量生物化合物，例如细菌、酶、激素等。

  公开号：

  US04600775A1

文献信息

• Quantification of hydrogen peroxyde by triggered reconstitution of horseradish peroxidase using a modified hemin
  申请人：Universität Heidelberg

  公开号：EP1990347A1

  公开（公告）日：2008-11-12

  The present invention relates to specific hemin derivatives, a kit comprising these hemin derivatives in combination with apo-horseradish peroxidase (apo-HRP), and an assay method for detecting and/or quantifying an analyte in a biological sample which comprises detecting hydrogen peroxide generated in the presence as opposed to the absence of said analyte by bringing said sample into contact with such a kit.

  本发明涉及特定的血红素衍生物，一种包含这些血红素衍生物与去乙酰辣根过氧化物酶（apo-HRP）结合的试剂盒，以及一种用于检测和/或定量生物样本中分析物的测定方法，该方法包括通过将样本与该试剂盒接触来检测在有分析物存在的情况下与不存在的情况相对生成的过氧化氢。
• ENZYME DETECTION/ASSAY METHOD AND SUBSTRATES
  申请人：——

  公开号：US20010019823A1

  公开（公告）日：2001-09-06

  The invention relates to a method of detecting and/or assaying nucleoside hydrolases or nucleoside phosphorylases using a chromogenic substrate. Preferred chromogenic substrates have formula (I) where X is OH, or H, and Y is the residue of Y—OH where Y—OH is a chromophore or a compound readily converted to a chromophore and the substrates are hydrolysed by the nucleoside hydrolase to yield ribose or 2-deoxyribose plus Y—OH. Alternatively those substrates may be phosphorylysed by nucleoside phosphorylase to yield ribose-1-phosphate plus Y—OH. The methods may be used to detect and/or assay parasites in biological samples.

  该发明涉及一种使用显色底物检测和/或测定核苷水解酶或核苷酸磷酸酶的方法。首选的显色底物具有式(I)，其中X为OH或H，Y为Y—OH的残基，其中Y—OH为色团或易于转化为色团的化合物，这些底物通过核苷水解酶水解产生核糖或2-脱氧核糖以及Y—OH。或者这些底物可能被核苷酸磷酸酶磷酸化产生核糖-1-磷酸加Y—OH。这些方法可用于检测和/或测定生物样本中的寄生虫。
• IMMUNOSUPPRESSIVE COMPOUNDS
  申请人：Mesaik Muhammad A.

  公开号：US20140378515A1

  公开（公告）日：2014-12-25

  The invention feature series of benzothiazole derivatives as potent immunosuppressive and antiinflammatory agents. Eight compounds 2, 4, 5, 8, 9, 10, 12, and 18 showed potent inhibitory activity on PHA-activated T-cell proliferation. Compounds 2, 4, 8, and 18 were found to have a potent inhibitory activity with IC 50 values ranging <1.0-2.9 μg/mL against IL-2. Studies on innate immune response revealed that compounds 2, 8, 9, and 10 have significant suppressive effect on ROS production with an IC 50 values 1.9, <1, 3.7 and 1.1 μg/mL, respectively. The LPS-induced nitrites in J774 macrophages cell line was inhibited by 4, 8, 9, and 18 at a concentration of 25 μg/mL (56-91%). In addition compounds 5, 8, 12, and 18 showed potent suppression on interleukin 4 (IL-4), particularly 9 (IC 50 <1 μg/mL). No cytotoxicity was found except for compound 9 and 18 (11.4 and 10.4 μg/mL IC 50 ), respectively.

  苯并噻唑衍生物系列的发明特征作为强效免疫抑制剂和抗炎剂。八种化合物2、4、5、8、9、10、12和18表现出对PHA激活的T细胞增殖具有强效的抑制活性。发现化合物2、4、8和18在IL-2上有强效的抑制活性，IC50值范围在<1.0-2.9 μg/mL之间。对先天免疫反应的研究显示，化合物2、8、9和10对ROS产生具有显著的抑制作用，其IC50值分别为1.9、<1、3.7和1.1 μg/mL。J774巨噬细胞系中LPS诱导的亚硝酸盐在25 μg/mL浓度下被化合物4、8、9和18抑制（56-91%）。此外，化合物5、8、12和18对白细胞介素4（IL-4）表现出强效的抑制作用，尤其是9（IC50<1 μg/mL）。除了化合物9和18（分别为11.4和10.4 μg/mL的IC50），未发现细胞毒性。
• Preparation of prodrugs for selective drug delivery
  申请人：Mills L. Randell

  公开号：US20050080260A1

  公开（公告）日：2005-04-14

  Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

  合成具有A-B-C化学式的化合物，可用于药物传递等应用，其中A是化学发光基团，B是光致变色基团，C是生物活性基团，其中A-B-C可作为前药。本发明的新型合成方法用于形成前药，包括以下步骤：(1)形成苯酮，(2)形成二芳基乙烯，(3)将邻苯二甲酰亚胺基团连接到乙烯的至少一个芳基上，形成邻苯二甲酰亚胺-乙烯共轭物，(4)缩合两个乙烯-邻苯二甲酰亚胺共轭物，形成邻苯二甲酰亚胺-戊二烯共轭物，(5)通过与肼反应将邻苯二甲酰亚胺转化为邻苯二酰肼，形成本发明的载体化合物，(6)将载体化合物与药物的亲核基团反应，形成相应的前药。另外，可以通过使用卤代二芳基乙烯制备相应的阳离子类似的类似类似染料化合物。然后，通过与亲核试剂反应保护阳离子类似化合物，并通过钯催化的胺化与氨基邻苯二甲酰亚胺偶联，形成保护的邻苯二甲酰亚胺-戊二烯共轭物。后者与肼回流，将其邻苯二甲酰亚胺转化为邻苯二酰肼，并酸化以得到载体。本发明的另一个方面涉及将这些化合物用作抗病毒剂，用于治疗病毒感染，如HIV，以及用作抗癌剂，用于治疗结肠癌、肺癌和乳腺癌等癌症。
• CRYSTALLINE FORMS FOR 5-AMINO-2, 3-DIHYDROPHTHALAZINE-1, 4-DIONE SODIUM SALT, PHARMACEUTICAL PREPARATIONS CONTAINING THE SAME AND METHOD FOR THE PRODUCTION OF SAID FORMS
  申请人：Breu Josef

  公开号：US20120329801A1

  公开（公告）日：2012-12-27

  The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both.

  本发明涉及为5-氨基-2,3-二氢鞣酸1,4-二酮钠盐提供两种新的晶体形式I和II。令人惊讶的是，发现I和II形式具有不同的免疫学效果。这种有利的性质对于免疫特异性应用非常有用。此外，这两种形式具有有利的物理化学性质，对于制备、进一步加工和/或使用I或II形式或两者的混合物的制药制剂非常有用。