2-氨基-5-(对甲苯)噻唑 | 73040-54-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 2-氨基-5-(对甲苯)噻唑
• 中文别名: 2-氨基-5-(对甲苯基)噻唑
• 英文名称: 5-(p-tolyl)thiazol-2-amine
• 英文别名: 5-p-tolyl-thiazol-2-ylamine；5-p-tolylthiazol-2-amine；5-(4-methylphenyl)-1,3-thiazol-2-amine
• CAS: 73040-54-7
• 化学式: C₁₀H₁₀N₂S
• mdl: MFCD00858269
• 分子量: 190.269
• InChiKey: BHSKUJCHFMAMKF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  67.2
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2934100090
• 储存条件：
  存放于惰性气体中，避免接触空气。

SDS

5-(对甲苯基)噻唑-2-胺MSDS英文版

反应信息

• 作为反应物：
  描述：

  3,4-二甲氧基苯甲醛 、 2-氨基-5-(对甲苯)噻唑 在 溶剂黄146 作用下， 以 甲醇 为溶剂， 反应 6.0h， 以99%的产率得到3,3'-((3,4-dimethoxyphenyl)methylene)bis(5-(p-tolyl)thiazol-2(3H)-imine)
  参考文献：
  名称：

  由2-氨基噻唑和醛类合成的新型底物控制的化学选择性合成芳基双（噻唑-2-亚胺）甲烷

  摘要：

  芳基双（噻唑-2-亚胺）甲烷是首次化学选择合成的，方法是在温和的条件下，使用廉价且易得的乙酸作为催化剂，通过5-芳基取代的2-氨基噻唑与芳香族醛类之间的异常反应，以优异的收率进行合成。本协议是通过缩合和亲核加成反应通过NC键形成而构建的。

  DOI：

  10.1016/j.tetlet.2017.06.068
• 作为产物：
  描述：

  硫脲 、 对甲基苯乙酮 在 磺酰氯 作用下， 生成 2-氨基-5-(对甲苯)噻唑
  参考文献：
  名称：

  Facile and efficient preparation of hybrid phenylthiazolyl-1,3,5-triazines and their antidepressant-like effect in mice

  摘要：

  DOI：

  10.1016/j.tetlet.2014.04.014

文献信息

• Modification and Biological Evaluation of Thiazole Derivatives as Novel Inhibitors of Metastatic Cancer Cell Migration and Invasion
  作者：Shilong Zheng、Qiu Zhong、Yulan Xi、Madhusoodanan Mottamal、Qiang Zhang、Richard L. Schroeder、Jayalakshmi Sridhar、Ling He、Harris McFerrin、Guangdi Wang

  DOI：10.1021/jm500724x

  日期：2014.8.14

  emerged as a potential therapeutic target, as its expression in cancer cells is closely associated with tumor progression and metastasis. Following the initial discovery of a series of thiazole derivatives that demonstrated potent antimigration and antiinvasion activities via possible inhibition of fascin function, we report here the design and synthesis of 63 new thiazole derivatives by further structural

  Fascin 最近已成为潜在的治疗靶点，因为它在癌细胞中的表达与肿瘤进展和转移密切相关。在最初发现一系列通过可能抑制肌成束蛋白功能而表现出有效抗迁移和抗侵袭活性的噻唑衍生物之后，我们在此报告了 63 种新型噻唑衍生物的设计和合成，通过进一步的结构修饰来寻找更有效的肌成束蛋白抑制剂。在噻唑氮上具有更长烷基链取代的5系列类似物比具有其他结构基序的类似物表现出更大的抗迁移活性。最强大的模拟，5p，在 24 nM 时抑制了 50% 的细胞迁移。此外，噻唑类似物显示出很强的抗血管生成活性，在鸡胚胎膜试验中阻断了新血管的形成。最后，进行了一项功能研究，以通过与 F-肌动蛋白捆绑蛋白肌成束蛋白的相互作用来研究作用机制。
• N-(METHYL) -1H-PYRAZOL-3-AMINE, N-(METHYL)-PYRIDIN-2-AMINE AND N-(METHYL)-THIAZOL-2-AMINE DERIVATIVES FOR THE TREATMENT OF DISEASES ASSOCIATED WITH AMYLOID OR AMYLOID-LIKE PROTEINS, LIKE E.G. ALZHEIMER'S
  申请人：Froestl Wolfgang

  公开号：US20100183513A1

  公开（公告）日：2010-07-22

  The present invention relates to novel compounds of formula (II) that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating, or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

  本发明涉及式（II）的新化合物，可用于治疗与淀粉样蛋白相关的一组紊乱和异常，如阿尔茨海默病，以及与淀粉样蛋白类似的蛋白质相关的疾病或病况。本发明的化合物还可用于治疗与视觉系统组织的病理性异常/变化相关的眼部疾病。本发明还涉及包含这些化合物的制药组合物，并且涉及使用这些化合物制备用于治疗或预防与淀粉样和/或淀粉样类似蛋白质相关的疾病或病况的药物。还公开了一种治疗或预防与淀粉样和/或淀粉样类似蛋白质相关的疾病或病况的方法。
• NOVEL COMPOUND FOR THE TREATMENT OF DISEASES ASSOCIATED WITH AMYLOID OR AMYLOID-LIKE PROTEINS
  申请人：FROESTL Wolfgang

  公开号：US20120309791A1

  公开（公告）日：2012-12-06

  The present invention relates to novel compounds of formula (II) that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating, or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed

  本发明涉及公式（II）的新化合物，可用于治疗与淀粉样蛋白相关的一组疾病和异常，例如阿尔茨海默病，以及与淀粉样蛋白类似蛋白质相关的疾病或病况。本发明的化合物还可用于治疗与视觉系统组织病理异常/变化相关的眼部疾病。本发明还涉及包含这些化合物的制药组合物以及使用这些化合物制备治疗或预防与淀粉样和/或淀粉样类似蛋白质相关的疾病或病况的药物的用途。还公开了一种治疗或预防与淀粉样和/或淀粉样类似蛋白质相关的疾病或病况的方法。
• Compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
  申请人：Froestl Wolfgang

  公开号：US08673940B2

  公开（公告）日：2014-03-18

  The present invention relates to novel compounds of formula (II) that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating, or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

  本发明涉及式（II）的新化合物，可用于治疗与淀粉样蛋白相关的一组疾病和异常，如阿尔茨海默病，以及与淀粉样蛋白类似蛋白质相关的疾病或病况。本发明的化合物还可用于治疗与视觉系统组织中的病理异常/变化相关的眼部疾病。本发明还涉及包含这些化合物的制药组合物，并且涉及使用这些化合物制备用于治疗或预防与淀粉样和/或淀粉样类似蛋白质相关的疾病或病况的药物。还公开了一种治疗或预防与淀粉样和/或淀粉样类似蛋白质相关的疾病或病况的方法。
• N-(methyl)-pyridin-2-amine derivatives for the treatment of diseases associated with amyloid or amyloid-like proteins
  申请人：AC Immune S.A.

  公开号：EP2108644A1

  公开（公告）日：2009-10-14

  The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

  本发明涉及可用于治疗与淀粉样蛋白相关的一组疾病和异常（如阿尔茨海默病）以及与淀粉样蛋白相关的疾病或病症的新型化合物。本发明的化合物还可用于治疗与视觉系统组织的病理异常/变化有关的眼部疾病。本发明进一步涉及包含这些化合物的药物组合物，以及这些化合物用于制备治疗或预防与淀粉样蛋白和/或淀粉样蛋白相关的疾病或病症的药物。还公开了一种治疗或预防与淀粉样蛋白和/或淀粉样蛋白相关的疾病或病症的方法。