2-[5-[[((2,6-二氯苯基)甲基]硫代]-1,3,4-噻二唑-2-基]吡嗪 | 448947-81-7

• 物质功能分类: 生物化工 - 生化试剂 - 激动剂抑制剂
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 2-[5-[[((2,6-二氯苯基)甲基]硫代]-1,3,4-噻二唑-2-基]吡嗪
• 英文名称: yoda1
• 英文别名: 2-[(2,6-Dichlorophenyl)methylsulfanyl]-5-pyrazin-2-yl-1,3,4-thiadiazole
• CAS: 448947-81-7
• 化学式: C₁₃H₈Cl₂N₄S₂
• 分子量: 355.271
• InChiKey: BQNXBSYSQXSXPT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  105
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  吡嗪-2-羧酸甲酯 在 potassium carbonate 、 一水合肼 、 potassium hydroxide 作用下， 以 乙醇 、 丙酮 为溶剂， 反应 8.5h， 生成 2-[5-[[((2,6-二氯苯基)甲基]硫代]-1,3,4-噻二唑-2-基]吡嗪
  参考文献：
  名称：

  10.1021/acs.jmedchem.4c00322

  摘要：

  DOI：

  10.1021/acs.jmedchem.4c00322

文献信息

• Heterocyclic inhibitors of glycine transporter 2
  申请人：——

  公开号：US20030073726A1

  公开（公告）日：2003-04-17

  Compounds, compositions, and methods for inhibiting the glycine transporter 2 and for inhibiting glycine transporter mediated neuronal activity. These compounds are particularly useful for treating diseases of the nerve and muscle, including psychoses, pain, epilepsy, neurodegenerative diseases, stroke, head trauma, multiple sclerosis and the like, and of muscle disorders, including diseases or conditions associated with increased muscle contraction, such as spasticity and myoclonus. In addition, the compounds may be used to discover other agents with improved activity in assays in which the compounds of the invention are active.

  用于抑制甘氨酸转运蛋白2和抑制甘氨酸转运蛋白介导的神经活动的化合物、组合物和方法。这些化合物特别适用于治疗神经和肌肉疾病，包括精神病、疼痛、癫痫、神经退行性疾病、中风、头部创伤、多发性硬化等，以及肌肉疾病，包括与肌肉过度收缩相关的疾病或症状，如痉挛和肌阵挛。此外，这些化合物可用于发现在这些化合物具有活性的检测中具有改进活性的其他药物。
• [EN] PIEZO1 AGONISTS FOR THE PROMOTION OF BONE FORMATION<br/>[FR] AGONISTES DE PIÉZO 1 POUR LA PROMOTION DE LA FORMATION OSSEUSE
  申请人：BIOVENTURES LLC

  公开号：WO2021067943A1

  公开（公告）日：2021-04-08

  Disclosed herein are Piezo 1 agonists. Also disclosed herein are methods of stimulating tissue anabolism in a subject comprising administering an effective amount of a Piezo 1 agonist and methods for chemically mimicking mechanical stimulation of a cell expressing Piezo 1 comprising contacting a cell expressing Piezo1 with an effective amount of a Piezo 1 agonist.

  本文披露了Piezo 1激动剂。本文还披露了一种在受试者中刺激组织合成的方法，包括给予有效量的Piezo 1激动剂，并且披露了一种化学模拟表达Piezo 1的细胞的机械刺激的方法，包括用有效量的Piezo 1激动剂接触表达Piezo1的细胞。
• HETEROCYCLIC INHIBITORS OF GLYCINE TRANSPORTER 2
  申请人：TELIK, INC.

  公开号：EP1357913A1

  公开（公告）日：2003-11-05
• METHODS FOR GENERATING HEMATOPOIETIC STEM CELLS
  申请人：The Brigham and Women's Hospital, Inc.

  公开号：EP3802790A2

  公开（公告）日：2021-04-14
• PIEZO AGONISTS FOR PREVENTING OR REVERTING ABNORMAL AMYLOID DEPOSITION
  申请人：ITÄ-SUOMEN YLIOPISTO

  公开号：US20220265646A1

  公开（公告）日：2022-08-25

  The present invention relates to diagnosing, preventing, delaying or reverting the progression of pathologies associated with abnormal amyloid deposits, such as that exemplified by Alzheimer's disease (AD). More specifically, the method involves administration of specific molecules that function as Piezo agonists, such as Yoda1, Jedi1, 5 Jedi2, or functional analogs thereof, that are able to modulate microglial activation towards anti-inflammatory state and/or interfere with the formation of amyloidogenic peptides and/or increase their efflux from the central nervous system. These agonists are applicable in disease states associated with, or at risk of, cerebral amyloidosis, such as AD, Parkinson's disease, stroke, head trauma(s), cerebral amyloid angiopathies, spongiform 10 encephalopathies and scrapie all of which are evidenced with abnormal proinflammatory microglial activation