安吡托林 | 98330-05-3

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 中文名称: 安吡托林
• 中文别名: 昂普托宁
• 英文名称: Anpirtoline
• 英文别名: 2-chloro-6-piperidin-4-ylsulfanylpyridine
• CAS: 98330-05-3
• 化学式: C₁₀H₁₃ClN₂S
• mdl: MFCD00868626
• 分子量: 228.74
• InChiKey: GGALEXMXDMUMDM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  50.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  BOC-甘氨酸 、 安吡托林 生成 (2S)-2-amino-1-[4-(6-chloropyridin-2-yl)sulfanylpiperidin-1-yl]propan-1-one
  参考文献：
  名称：

  ENGEL, JURGEN;KLEEMANN, AXEL;NICKEL, BERND;SZELENYI, ISTVAN

  摘要：

  DOI：
• 作为产物：
  描述：

  1-N-boc-4-疏基哌啶 在 三乙基硅烷 、 potassium carbonate 、 三氟乙酸 作用下， 以 二氯甲烷 、 异丙醇 为溶剂， 生成 安吡托林
  参考文献：
  名称：

  多峰吖啶光催化能够直接从羧酸和元素硫中获取硫醇

  摘要：

  开发光催化系统，通过不同的激活模式促进复杂催化歧管中机械上不同的步骤，可以实现以前无法实现的合成转化。然而，多模态光催化系统仍未得到充分研究，阻碍了其在催化方法中的实施。我们在此报告了一种光催化获得硫醇的方法，该方法直接将羧酸的结构多样性与元素硫的现成可用性相结合，而无需底物预活化。光催化转化为生物学上最重要和合成上最通用的有机硫功能之一提供了直接的自由基介导的序列，其合成可及性仍然主要由基于有毒且不经济的试剂和前体的双电子介导的过程主导。吖啶光催化的多峰催化反应性促进了两相自由基过程，该反应性既能够形成单线态激发态PCET介导的脱羧碳硫键，又能够通过硅烷中的光诱导氢原子转移过程实现先前未知的自由基还原二硫键断裂。三重态吖啶系统。该研究指出多模态光催化系统在为以前无法​​实现的转化提供未探索的方向方面具有巨大的潜力。

  DOI：

  10.1021/acscatal.4c01289

文献信息

• PYRIDIN-2YL SULFANYL ACID ESTERS AND PROCESS FOR THE PREPARATION THEREOF
  申请人：Sarma Jadab Chandra

  公开号：US20130131350A1

  公开（公告）日：2013-05-23

  The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R 1 =H, R 2 =H, R 3 =CH2-COOC5H 11 ) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.

  本发明涉及具有抗炎性能的吡啶-2-基硫醇酸酯化合物。本发明特别涉及吡啶-2-基硫醇的新型抗炎杂环酸酯，其具有通式1的结构，已经针对其抗炎活性进行了筛选，以抑制从人类外周血液中分离出的中性粒细胞粘附到人脐静脉内皮细胞（HU-VEC）表面，结果是通过抑制细胞粘附分子ICAM-1的细胞因子刺激表达来实现。化合物RS—Z，3-(吡啶-2-基硫醇)-丙酸戊酯（结构1a，R1=H，R2=H，R3=CH2-COOC5H11）被发现对ICAM-1和中性粒细胞粘附抑制效果最显著，并且被发现有效缓解由过度白细胞浸润引起的炎症，导致炎症性疾病或类似症状，如小鼠的急性肺损伤和急性呼吸窘迫综合征。
• [EN] PYRIDIN- 2 - YL SULFANYL ACID ESTERS AND PROCESS FOR THE PREPARATION THEREOF<br/>[FR] ESTERS DE PYRIDIN-2-YLSULFANYLACIDES ET LEUR PROCÉDÉ DE SYNTHÈSE
  申请人：COUNCIL SCIENT IND RES

  公开号：WO2012011123A1

  公开（公告）日：2012-01-26

  The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HUVEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS-Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure la, R1 = H, R2 = H, R3 = CH2COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.

  本发明涉及具有抗炎性质的吡啶-2-基巯酸酯化合物。本发明特别涉及一类新型的抗炎杂环酸酯，其具有通用公式1的结构，并且已经通过抑制从人外周血中分离的中性粒细胞粘附到人脐静脉内皮细胞（HUVEC）表面的能力来筛选其抗炎活性，这是通过抑制细胞粘附分子ICAM-1的细胞因子刺激表达的结果。发现化合物RS-Z，3-(吡啶-2-基巯基)-丙酸戊酯（结构la，R1 = H，R2 = H，R3 = CH2COOC5H11）对ICAM-1和中性粒细胞粘附抑制最有效，并且发现它有效地缓解了由过度白细胞浸润导致的炎症介导的炎症疾病或类似状况，例如小鼠的急性肺损伤和急性呼吸窘迫综合征。
• 1-(2-m-methanesulfonamidophenylethyl)-4-(m-trifluoromethylphenyl) piperazine and pharmaceutically acceptable salts and solvents thereof
  申请人：——

  公开号：US20040067962A1

  公开（公告）日：2004-04-08

  The present invention provides a compound of the formula (I), and the pharmaceutically acceptable salts and solvates thereof, which is useful for treating bladder over-activity or urinary incontinence.

  本发明提供了一种符合式(I)的化合物，以及其药用可接受的盐和溶剂合物，用于治疗膀胱过度活动或尿失禁。
• Carbamoyl esters that inhibit cholinesterase and release pharmacologically active agents
  申请人：Verheijen C. Jeroen

  公开号：US20050096387A1

  公开（公告）日：2005-05-05

  Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

  碳酰基酯抑制胆碱酯酶活性，水解后释放出药理活性成分。在一种实施例中，碳酰基酯具有以下结构：其中A选自无取代芳基、取代芳基、无取代杂环芳基和取代杂环芳基的群组。碳酰基酯用于治疗个体的方法中。通过水解碳酰基酯获得的药理活性成分可以治疗例如神经系统疾病、胆碱能缺乏以及与药理活性成分缺乏相关的疾病或病症，例如乙酰胆碱。
• Sigma ligands for use in the prevention and/or treatment of postoperative pain
  申请人：Laboratorios del. Dr. Esteve, S.A.

  公开号：EP2353598A1

  公开（公告）日：2011-08-10

  The invention refers to the use of a sigma ligand, particularly a sigma ligand of formulae (I), (II) or (III) to prevent and/or treat acute and chronic pain developed as a consequence of surgery, especially superficial and/or deep pain secondary to surgical tissue injury, and peripheral neuropathic pain, neuralgia, allodynia, causalgia, hyperalgesia, hyperesthesia, hyperpathia, neuritis or neuropathy secondary to surgical procedure.

  本发明涉及使用sigma配体，特别是公式（I），（II）或（III）的sigma配体，以预防和/或治疗由手术引起的急性和慢性疼痛，特别是手术组织损伤引起的表浅和/或深层疼痛，以及周围神经病理性疼痛，神经痛，触痛，烧伤性痛，痛觉过敏，疼痛过敏，神经炎或手术过程引起的神经病变。