8H-indeno[1,2-d]thiazol-2-ylamine hydroiodid

• 分子结构分类: 有机化合物 - 苯类化合物
• 英文名称: 8H-indeno[1,2-d]thiazol-2-ylamine hydroiodid
• 英文别名: 8H-Indeno[1,2-d]thiazol-2-ylamine hydroiodide；4H-indeno[1,2-d][1,3]thiazol-2-amine;hydroiodide
• 化学式: C₁₀H₈N₂S*HI
• 分子量: 316.165
• InChiKey: PKJLOKWROSJRTD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.91
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  67.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  8H-indeno[1,2-d]thiazol-2-ylamine hydroiodid 在 水 作用下， 以 sodium hydroxide 为溶剂， 反应 1.0h， 以to provide 5.30 g of 8H-Indeno[1,2-d]thiazol-2-ylamine 1b的产率得到8H-茚并[1,2-d]噻唑-2-胺
  参考文献：
  名称：

  Substituted N-acyl-2-aminothiazoles

  摘要：

  提供了公式或其药学上可接受的盐的化合物，可用于治疗糖尿病、糖尿病视网膜病变、哮喘和腹泻。

  公开号：

  US07407977B2
• 作为产物：
  描述：

  1-茚酮 、 硫脲 在 碘 作用下， 反应 3.0h， 生成 8H-indeno[1,2-d]thiazol-2-ylamine hydroiodid
  参考文献：
  名称：

  Substituted N-acyl-2-aminothiazoles

  摘要：

  提供了该公式化合物或其药用可接受的盐，可用于治疗糖尿病、糖尿病视网膜病变、哮喘和腹泻。

  公开号：

  US20060030589A1

文献信息

• 2-Aminothiazoles: A new class of agonist allosteric enhancers of A1 adenosine receptors
  作者：Mahendra D. Chordia、Lauren J. Murphree、Timothy L. Macdonald、Joel Linden、Ray A. Olsson

  DOI：10.1016/s0960-894x(02)00236-6

  日期：2002.6

  This report describes the synthesis and structure-activity relationships of a new class of A(1) adenosine receptor agonist allosteric enhancers, 2-aminothiazolium salts. The EC50 of compounds 6a, 6b, 7, and 8 were 0.3, 4.5, 3.8, and 1.2 muM, substantially lower than that of the 'Gold Standard' 2-amino-3-benzoyl thiophene (PD 81,723), which has an EC50 of 38 muM. (C) 2002 Elsevier Science Ltd. All rights reserved.
• Synthesis and biological evaluation of 2-aminothiazoles and their amide derivatives on human adenosine receptors. Lack of effect of 2-aminothiazoles as allosteric enhancers
  作者：Anikó Göblyös、Sabrina Neves Santiago、Daniele Pietra、Thea Mulder-Krieger、Jacobien von Frijtag Drabbe Künzel、Johannes Brussee、Adriaan P. IJzerman

  DOI：10.1016/j.bmc.2005.01.006

  日期：2005.3

  A number of 2-aminothiazoles (2a-e) and their amide derivatives (4-10) were prepared. The 2-aminothiazoles themselves were tested as allosteric enhancers of agonist binding to human adenosine A, receptors. In a variety of experimental set-ups the compounds did not show any such effect, in contrast to earlier findings by another research group. Subsequently the 2-aminothiazoles were used as intermediates in the synthesis of a number of amide derivatives of either aromatic (4-6) or aliphatic nature (7-10). Some of the compounds emerged as moderately active antagonists on human adenosine A(1) and/or A(2A) receptors with lower or negligible potency at adenosine A(3) receptors. (c) 2005 Elsevier Ltd. All rights reserved.
• SUBSTITUTED N-ACYL-2-AMINOTHIAZOLES
  申请人：F.HOFFMANN-LA ROCHE AG

  公开号：EP1791822A1

  公开（公告）日：2007-06-06
• US7407977B2
  申请人：——

  公开号：US7407977B2

  公开（公告）日：2008-08-05
• [EN] SUBSTITUTED N-ACYL-2-AMINOTHIAZOLES<br/>[FR] AMINOTHIAZOLES SUBSTITUÉS N-ACYLE-2-
  申请人：HOFFMANN LA ROCHE

  公开号：WO2006013054A1

  公开（公告）日：2006-02-09

  The invention is concerned with novel substituted N-acyl-2-aminothiazoles of the formula (I) wherein R, Ri and X are as defined in the specification and claims, as well as pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.