2,3,3a,4,5,6-六氢-1H-吡嗪并[3,2,1-JK]咔唑 | 18046-23-6

• 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
• 中文名称: 2,3,3a,4,5,6-六氢-1H-吡嗪并[3,2,1-JK]咔唑
• 英文名称: 2,3,3a,4,5,6-hexahydro-1H-pyrazino[3,2,1-jk]carbazole
• 英文别名: Piperazino<1,2-a>indol；Hexahydro-pyrazino-carbazol；1,2,3,4-Tetrahydro-1,10-trimethylen-pyrazino<1,2-a>-indol；1,4-diazatetracyclo[7.6.1.05,16.010,15]hexadeca-9(16),10,12,14-tetraene
• CAS: 18046-23-6
• 化学式: C₁₄H₁₆N₂
• 分子量: 212.294
• InChiKey: FPJQYYCGLQSBMU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  16
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  17
• 氢给体数：
  1
• 氢受体数：
  1

安全信息

• 危险等级：
  IRRITANT

反应信息

• 作为反应物：
  描述：

  氯乙酰胺 、 2,3,3a,4,5,6-六氢-1H-吡嗪并[3,2,1-JK]咔唑 以72%的产率得到
  参考文献：
  名称：

  DENKOVA, E.;STEFANOVA, D.;BIKOVA, N.;DALEVA, L.;VANKOV, S.;MARKOVA, S.;GR+, FARMATSIYA, NRB, 1982, 32, N 3, 1-6

  摘要：

  DOI：
• 作为产物：
  描述：

  1,2,3,4-四氢咔唑 在 sodium tetrahydroborate 、 五氧化二碘 、 五氯化磷 、 potassium carbonate 、 calcium carbonate 作用下， 以 四氢呋喃 、 甲醇 、 水 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 22.5h， 生成 2,3,3a,4,5,6-六氢-1H-吡嗪并[3,2,1-JK]咔唑
  参考文献：
  名称：

  NB 06: From a simple lysosomotropic aSMase inhibitor to tools for elucidating the role of lysosomes in signaling apoptosis and LPS-induced inflammation

  摘要：

  Ceramide generation is involved in signal transduction of cellular stress response, in particular during stress-induced apoptosis in response to stimuli such as minimally modified Low-density lipoproteins, TNFalpha and exogenous C-6-ceramide. In this paper we describe 48 diverse synthetic products and evaluate their lysosomotropic and acid sphingomyelinase inhibiting activities in macrophages. A stimuli induced increase of C-16-ceramide in macrophages can be almost completely suppressed by representative compound NB 06 providing an effective protection of macrophages against apoptosis. Compounds like NB 06 thus offer highly interesting fields of application besides prevention of apoptosis of macrophages in atherosclerotic plaques in vessel walls. Most importantly, they can be used for blocking pH dependent lysosomal processes and enzymes in general as well as for analyzing lysosomal dependent cellular signaling. Modulation of gene expression of several prominent inflammatory messengers IL1B, IL6, IL23A, CCL4 and CCL20 further indicate potentially beneficial effects in the field of (systemic) infections involving bacterial endotoxins like LPS or infections with influenza A virus. (C) 2017 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2017.09.021

文献信息

• TRIAZOLE DERIVATIVES FOR TREATING ALZHEIMER'S DISEASE AND RELATED CONDITIONS
  申请人：Fischer Christian

  公开号：US20100222320A1

  公开（公告）日：2010-09-02

  Compounds of formula I: Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain, in particular Alzheimer's disease.

  公式为I的化合物：选择性地减弱Aβ（1-42）的产生，因此可用于治疗或预防与Aβ在大脑中沉积相关的疾病，特别是阿尔茨海默病。
• GATTA F.; CHIAVARELLI S., FARMACO, ED. SCI. <FRPS-AX>, 1975, 30, NO 8, 631-641
  作者：GATTA F.、 CHIAVARELLI S.

  DOI：——

  日期：——
• ZUSAMMENSETZUNG ZUR TOPISCHEN BEHANDLUNG VON NICHT-MIKROORGANISMUS-VERURSACHTEN ENTZÜNDLICHEN HAUT- UND SCHLEIMHAUTERKRANKUNGEN
  申请人：Bläss, Markus

  公开号：EP3675814A1

  公开（公告）日：2020-07-08
• COMPOSITIONS AND METHODS FOR SELECTIVE DELIVERY OF OLIGONUCLEOTIDE MOLECULES TO CELL TYPES
  申请人：NLIFE THERAPEUTICS, S.L.

  公开号：US20150315575A1

  公开（公告）日：2015-11-05

  The invention provides a conjugate comprising (i) a nucleic acid which is complementary to a target nucleic acid sequence and which expression prevents or reduces expression of the target nucleic acid and (ii) a selectivity agent which is capable of binding with high affinity to a receptor which can be internalised by the cell in response to the binding of said selectivity agent. The conjugates of the present invention are useful for the delivery of the nucleic acid to cell of interests and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of contrast agents to the cells for diagnostic purposes.
• US8242150B2
  申请人：——

  公开号：US8242150B2

  公开（公告）日：2012-08-14