2-aminophenyl-2'-thiazolylketone | 39254-87-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-aminophenyl-2'-thiazolylketone
• 英文别名: (2-amino-phenyl)-thiazol-2-yl-methanone；(2-aminophenyl)(thiazol-2-yl)methanone；2-Aminophenyl 2-thiazolyl-ketone；2-aminophenyl 2-thiazolyl ketone；2-(2-aminobenzoyl)thiazole；o-Aminophenyl-thiazol-2-yl-keton；(2-aminophenyl)-(1,3-thiazol-2-yl)methanone
• CAS: 39254-87-0
• 化学式: C₁₀H₈N₂OS
• 分子量: 204.252
• InChiKey: KBQLILZTNFQUGU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  84.2
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-aminophenyl-2'-thiazolylketone 在 titanium(III) chloride 、 乙酸酐 、 锌 作用下， 以 乙二醇二甲醚 为溶剂， 反应 0.33h， 生成 camalexin
  参考文献：
  名称：

  卡那新，吲哚吡咯啉和黄酮哌丁胺的合成

  摘要：

  到植物抗毒素camalexin的短的合成路线7和会聚的方法来生物碱indolopyridocoline 8，6,7- dihydroflavopereirine 15和flavopereirine 9被呈现。从容易获得的前体开始，这些总的合成突出了基于低价钛诱导的氧代酰胺的还原形成C2 lowC3键的吲哚合成新方法的制备潜力。

  DOI：

  10.1016/0040-4020(94)00987-6
• 作为产物：
  描述：

  camalexin 在 sodium hydroxide 、 间氯过氧苯甲酸 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 26.0h， 生成 2-aminophenyl-2'-thiazolylketone
  参考文献：
  名称：

  Biotransformation of the phytoalexin camalexin by the phytopathogen Rhizoctonia solani

  摘要：

  The unusual metabolism of the cruciferous phytoalexin camalexin by virulent and weakly virulent isolates of the root rot fungus Rhizoctonia solani Kuhn is reported. This biotransformation proceeded via 5-hydroxycamalexin, which was further biotransformed into more polar metabolites. Importantly, the metabolites resulting from transformation of camalexin were significantly less toxic to the pathogen than camalexin. Thus, it was concluded that R. solani can detoxify camalexin through oxidation of the indole ring. The chemistry involved in the structure determination of the intermediates of this pathway, their synthesis as well as antifungal activity is described. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0031-9422(99)00479-3

文献信息

• Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
  申请人：——

  公开号：US20020045747A1

  公开（公告）日：2002-04-18

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  公开了抑制β-淀粉样肽释放和/或其合成的化合物，因此可用于治疗阿尔茨海默病。还公开了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这些药物组合物预防性和治疗性治疗阿尔茨海默病的方法。
• Cyclic amino acid compounds pharmaceutical compositions comprising same and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds
  申请人：Elan Pharmaceuticals, Inc.

  公开号：US06528505B1

  公开（公告）日：2003-03-04

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  公开了抑制β-淀粉样肽释放和/或其合成的化合物，因此可用于治疗阿尔茨海默病。还公开了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这些药物组合物预防性和治疗性治疗阿尔茨海默病的方法。
• [EN] AMIDE DERIVATIVES AS SIRTUIN MODULATORS<br/>[FR] DÉRIVÉS D'AMIDE COMME MODULATEURS DE SIRTUINES
  申请人：SIRTRIS PHARMACEUTICALS INC

  公开号：WO2009058348A1

  公开（公告）日：2009-05-07

  Provided herein are novel sirtuin-modulating compounds represented by Structural Formula (I) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin- modulating compound in combination with another therapeutic agent.

  提供的是由结构公式（I）表示的新的sirtuin调节化合物及其用途。sirtuin调节化合物可用于延长细胞寿命，以及治疗和/或预防多种疾病和紊乱，例如与衰老或压力、糖尿病、肥胖、神经退行性疾病、心血管疾病、凝血障碍、炎症、癌症和/或潮红相关的疾病或紊乱，以及将从增加线粒体活性中受益的疾病或紊乱。还提供了包含sirtuin调节化合物与另一种治疗剂的组合的药物组合物。
• Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting &bgr;-amyloid peptide release and/or its synthesis by use of such compounds
  申请人：Elan Pharmaceuticals, Inc.

  公开号：US06509331B1

  公开（公告）日：2003-01-21

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  公开了抑制β-淀粉样肽释放和/或其合成的化合物，因此可用于治疗阿尔茨海默病。还公开了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这些药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。
• Quinazolines and 1,4-benzodiazepines LXVIII. 5-Heterocyclic-substituted benzodiazepinones
  作者：Robert Kalish、E. Broger、George F. Field、T. Anion、Thomas V. Steppe、Leo H. Sternbach

  DOI：10.1002/jhet.5570120109

  日期：1975.2

  The synthesis of a number of new 1,4-benzodiazepin-2-ones containg the 2-thiazolyl, 5-isothiazolyl, 1-rnethyl-2-imidazolyl. 1-methyl-5-pyrazolyl, and 3,5-dimethyl-4-isoxazolyl groups in the 5-position of the benzodiazepine ring are described.

  包含2-噻唑基，5-异噻唑基，1-甲基-2-咪唑基的许多新的1,4-苯并二氮杂-2-酮的合成。描述了在苯并二氮杂ring环的5-位上的1-甲基-5-吡唑基和3，5-二甲基-4-异恶唑基。