5-thiazolidin-3-yl-pentylamine | 67855-29-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: 5-thiazolidin-3-yl-pentylamine
• 英文别名: 5-(1,3-Thiazolidin-3-yl)pentan-1-amine
• CAS: 67855-29-2
• 化学式: C₈H₁₈N₂S
• 分子量: 174.31
• InChiKey: DOMUFGJQXKVDRL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  11
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  54.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-thiazolidin-3-yl-pentylamine 在 碘 作用下， 以 异戊醇 、 氯仿 为溶剂， 反应 74.0h， 生成 2-N-[5-[2-[2-[5-[(4-amino-6,7-dimethoxyquinazolin-2-yl)amino]pentylamino]ethyldisulfanyl]ethylamino]pentyl]-6,7-dimethoxyquinazoline-2,4-diamine
  参考文献：
  名称：

  Synthesis and α1-antagonist activity of new prazosin- and benextramine-related tetraamine disulfides

  摘要：

  Tetraamine disulfides 1-10 were designed by combining the structural features of benextramine, an irreversible alpha(1)/alpha(2)-adrenoceptor antagonist, and prazosin, a selective competitive alpha(1)-antagonist. Their biological profile was assessed by functional and binding assays. In rat vas deferens functional experiments, tetraamine disulfides 1-10 displayed a marked selectivity at alpha(1)-adrenoceptors. Furthermore, they acted as competitive antagonists at alpha(1)-adrenoceptors and weak noncompetitive (irreversible) antagonists at alpha(2)-adrenoceptors. In binding assays, performed at alpha(1)-adrenoceptors of rat liver (alpha 1B) and submaxillary gland (alpha(1A), compound 5 showed an 11-fold selectivity for alpha(1B)-adrenoceptors in contrast to both prazosin and benextramine, which were not selective or selective for the alpha(1A)-subtype respectively.

  DOI：

  10.1016/s0223-5234(97)84357-7
• 作为产物：
  描述：

  聚合甲醛 、 以 水 为溶剂， 以60%的产率得到5-thiazolidin-3-yl-pentylamine
  参考文献：
  名称：

  Synthesis and α1-antagonist activity of new prazosin- and benextramine-related tetraamine disulfides

  摘要：

  Tetraamine disulfides 1-10 were designed by combining the structural features of benextramine, an irreversible alpha(1)/alpha(2)-adrenoceptor antagonist, and prazosin, a selective competitive alpha(1)-antagonist. Their biological profile was assessed by functional and binding assays. In rat vas deferens functional experiments, tetraamine disulfides 1-10 displayed a marked selectivity at alpha(1)-adrenoceptors. Furthermore, they acted as competitive antagonists at alpha(1)-adrenoceptors and weak noncompetitive (irreversible) antagonists at alpha(2)-adrenoceptors. In binding assays, performed at alpha(1)-adrenoceptors of rat liver (alpha 1B) and submaxillary gland (alpha(1A), compound 5 showed an 11-fold selectivity for alpha(1B)-adrenoceptors in contrast to both prazosin and benextramine, which were not selective or selective for the alpha(1A)-subtype respectively.

  DOI：

  10.1016/s0223-5234(97)84357-7

文献信息

• Ueda; Melchiorre; Lippert, Farmaco, Edizione Scientifica, 1978, vol. 33, # 7, p. 479 - 495
  作者：Ueda、Melchiorre、Lippert、Belleau、Chona、Triggle

  DOI：——

  日期：——
• METHOD FOR THE IMPROVEMENT OF ISLET SIGNALING IN DIABETES MELLITUS AND FOR ITS PREVENTION
  申请人：Royalty Pharma Collection Trust

  公开号：EP1283735B2

  公开（公告）日：2012-10-24
• Method for the improvement of islet signaling in diabetes mellitus and for its prevention
  申请人：Royalty Pharma Collection Trust

  公开号：EP2055302B1

  公开（公告）日：2014-09-10
• Synthesis and α1-antagonist activity of new prazosin- and benextramine-related tetraamine disulfides
  作者：D Giardinà、M Crucianelli、U Gulini、G Marucci、C Melchiorre、S Spampinato

  DOI：10.1016/s0223-5234(97)84357-7

  日期：1997.1

  Tetraamine disulfides 1-10 were designed by combining the structural features of benextramine, an irreversible alpha(1)/alpha(2)-adrenoceptor antagonist, and prazosin, a selective competitive alpha(1)-antagonist. Their biological profile was assessed by functional and binding assays. In rat vas deferens functional experiments, tetraamine disulfides 1-10 displayed a marked selectivity at alpha(1)-adrenoceptors. Furthermore, they acted as competitive antagonists at alpha(1)-adrenoceptors and weak noncompetitive (irreversible) antagonists at alpha(2)-adrenoceptors. In binding assays, performed at alpha(1)-adrenoceptors of rat liver (alpha 1B) and submaxillary gland (alpha(1A), compound 5 showed an 11-fold selectivity for alpha(1B)-adrenoceptors in contrast to both prazosin and benextramine, which were not selective or selective for the alpha(1A)-subtype respectively.