2-hydrazinoindolenine | 86691-39-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 2-hydrazinoindolenine
• 英文别名: 2-Hydrazinyl-3H-indole；3H-indol-2-ylhydrazine
• CAS: 86691-39-6
• 化学式: C₈H₉N₃
• mdl: MFCD12924154
• 分子量: 147.18
• InChiKey: QXDFTCMHNDXVPZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.125
• 拓扑面积：
  50.4
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  丙烯腈 、 2-hydrazinoindolenine 在 sodium hydroxide 作用下， 以 四氢呋喃 为溶剂， 生成 3-[1-(2-indolenyl)hydrazino]propanenitrile
  参考文献：
  名称：

  3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation

  摘要：

  3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives were evaluated in the dermal and pleural reverse passive Arthus reactions in the rat. In the pleural test these compounds were effective in reducing exudate volume and accumulation of white blood cells. This pattern of activity was similar to that of hydrocortisone and different from that of indomethacin. The structural requirements for inhibiting the Arthus reactions were studied by systematic chemical modification of 1. These structure-activity relationship studies revealed that nitrogen 1' of the hydrazino group is essential for activity and must be electron rich, whereas chemical modifications of other sites of 1 had only a modest effect on activity.

  DOI：

  10.1021/jm00117a010
• 作为产物：
  描述：

  2-吲哚酮 在 一水合肼 、 三乙胺 、 三氯氧磷 作用下， 生成 2-hydrazinoindolenine
  参考文献：
  名称：

  3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation

  摘要：

  3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives were evaluated in the dermal and pleural reverse passive Arthus reactions in the rat. In the pleural test these compounds were effective in reducing exudate volume and accumulation of white blood cells. This pattern of activity was similar to that of hydrocortisone and different from that of indomethacin. The structural requirements for inhibiting the Arthus reactions were studied by systematic chemical modification of 1. These structure-activity relationship studies revealed that nitrogen 1' of the hydrazino group is essential for activity and must be electron rich, whereas chemical modifications of other sites of 1 had only a modest effect on activity.

  DOI：

  10.1021/jm00117a010

文献信息

• BENZOTHIAZOLE COMPOUNDS
  申请人：Watson Keith Geoffrey

  公开号：US20100197711A1

  公开（公告）日：2010-08-05

  The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival.

  本发明涉及苯并噻唑化合物，其模拟BH3仅蛋白的活性，并能够结合和中和促生存的Bcl-2蛋白。本发明还涉及使用这种化合物来调节细胞死亡或细胞存活以及治疗和/或预防与细胞死亡或细胞存活失调相关的疾病或病症。
• HAVIV, FORTUNA;RATAJCZYK, JAMES D.;DENET, ROBERT W.;KERDESKY, FRANCIS A.;+, J. MED. CHEM., 31,(1988) N 9, C. 1719-1728
  作者：HAVIV, FORTUNA、RATAJCZYK, JAMES D.、DENET, ROBERT W.、KERDESKY, FRANCIS A.、+

  DOI：——

  日期：——
• (1-(2-BENZOXAZOLYL)HYDRAZINO)ALKYL NITRILE DERIVATIVES
  申请人：ABBOTT LABORATORIES

  公开号：EP0091468A1

  公开（公告）日：1983-10-19
• EP0091468A4
  申请人：——

  公开号：EP0091468A4

  公开（公告）日：1985-07-01
• [EN] [1-(2-BENZOXAZOLYL)HYDRAZINO]ALKYL NITRILE DERIVATIVES
  申请人：ABBOTT LABORATORIES

  公开号：WO1983001448A1

  公开（公告）日：1983-04-28

  (EN) Described are compounds of the formula$(10,)$wherein R is hydrogen or loweralkyl, X and Y independently of one another denote hydrogen, halogen, loweralkyl, nitro, amino, amido, loweralkoxy, hydroxy, nitrile, methylsulfone, methylsulfoxide, methylmercapto, trifluoromethyl or benzyloxy; Z is oxygen, sulfur or -CH2; n and m are each an integer from 0 to 6 inclusive, and pharmaceutically acceptable salts thereof. The compounds are effect as anti-inflammatory agents. (FR) Sont décrits les composés correspondant à la formule:$(10,)$où R est un hydrogène ou un alkyl inférieur, X et Y représentent indépendamment l'un de l'autre un hydrogène, un halogène, un alkyl inférieur, un nitro, un amino, un amido, un alkoxy inférieur, un hydroxy, un nytril, une méthylsulfone, un méthylsulfoxyde, un méthylmercapto, un trifluorométhyl ou un benzyloxy; Z représente l'oxygène, le soufre ou -CH2; n et m sont chacun un nombre entier compris entre 0 et 6 inclusivement, et leurs sels pharmaceutiquement acceptables. Ces composés sont efficaces en tant qu'agent anti-inflammatoires.