2-Hydrazino-2-thiazoline | 45439-41-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑啉类
• 英文名称: 2-Hydrazino-2-thiazoline
• 英文别名: 2-thiazolinylhydrazine；thiazolidin-2-one hydrazone；2-Hydrazino-2-thiazolin；4,5-dihydro-1,3-thiazol-2-ylhydrazine
• CAS: 45439-41-6
• 化学式: C₃H₇N₃S
• mdl: MFCD00140892
• 分子量: 117.175
• InChiKey: ODJMVCUWUNEOTJ-UHFFFAOYSA-N

物化性质

• 沸点：
  243.2±23.0 °C(Predicted)
• 密度：
  1.61±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  7
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.666
• 拓扑面积：
  75.7
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-Hydrazino-2-thiazoline 生成 1,1'-(Dithiodiaethylen)-2,2'-bis-
  参考文献：
  名称：

  2-Amino-2-thiazoline. IV. Ring-opening of 2-amino-2-thiazolines and 2-amino-2-selenazoline with hydrogen sulfide to form thiourea derivatives

  摘要：

  DOI：

  10.1021/jo01266a102
• 作为产物：
  描述：

  2-Hydrazino-2-thiazolin-hydrobromid 在 sodium 作用下， 以 乙醇 为溶剂， 反应 0.08h， 生成 2-Hydrazino-2-thiazoline
  参考文献：
  名称：

  Ongania, Karl-Hans, Chemische Berichte, 1981, vol. 114, # 3, p. 1200 - 1202

  摘要：

  DOI：

文献信息

• Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
  作者：Kim K. Adkison、David G. Barrett、David N. Deaton、Robert T. Gampe、Anne M. Hassell、Stacey T. Long、Robert B. McFadyen、Aaron B. Miller、Larry R. Miller、J. Alan Payne、Lisa M. Shewchuk、Kevin J. Wells-Knecht、Derril H. Willard、Lois L. Wright

  DOI：10.1016/j.bmcl.2005.10.108

  日期：2006.2

  Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.
• The Serotonin 5-HT4 Receptor. 2. Structure-Activity Studies of the Indole Carbazimidamide Class of Agonists
  作者：Karl-Heinz Buchheit、Rainer Gamse、Rudolf Giger、Daniel Hoyer、Francois Klein、Edgar Kloeppner、Hans-Juergen Pfannkuche、Henri Mattes

  DOI：10.1021/jm00013a010

  日期：1995.6

  A number of substituted indole carbazimidamides were prepared and evaluated as 5-HT4 receptor agonists by using the isolated field-stimulated guinea pig ileum preparation. Their selectivity for the 5-HT4 receptor was established by examining their affinity for other 5-HT receptors using radioligand-binding techniques. Several selective and highly potent full as well as partial agonists emerged from this study. For example, 1b,d were found to be the most potent, full 5-HT4 receptor agonists described so far (EC(50) = 0.5 and 0.8 nM, respectively), being 6 and 4 times more potent than serotonin itself. On the other hand, 5b and 1h appeared as partial 5-HT4 receptor agonists in the nonstimulated guinea pig ileum preparation with potencies, evaluated against serotonin action, respectively similar (5b, K-i = 12 nM) to and 300-fold higher (1h, K-i = 0.04 nM) than serotonin.
• Cavalleri; Volpe; Ripamonti, Arzneimittel-Forschung/Drug Research, 1977, vol. 27, # 6, p. 1131 - 1134
  作者：Cavalleri、Volpe、Ripamonti、Arioli

  DOI：——

  日期：——
• 2-Hydrazino- and 2-(2,2-Dimethylhydrazino)-2-thiazoline¹
  作者：Thomas P. Johnston、Carl R. Stringfellow、Anne Gallagher

  DOI：10.1021/jo01017a519

  日期：1965.6
• ONGANIA K.-H., CHEM. BER., 1981, 114, NO 3, 1200-1202
  作者：ONGANIA K.-H.

  DOI：——

  日期：——