N-(5-异丙基-1,3-噻唑-2-基)-2-苯基乙酰胺 | 267654-00-2

• 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: N-(5-异丙基-1,3-噻唑-2-基)-2-苯基乙酰胺
• 英文名称: BML-259
• 英文别名: 2-phenyl-N-(5-propan-2-yl-2-thiazolyl)acetamide；2-phenyl-N-(5-propan-2-yl-1,3-thiazol-2-yl)acetamide
• CAS: 267654-00-2
• 化学式: C₁₄H₁₆N₂OS
• 分子量: 260.36
• InChiKey: IGRZXNLKVUEFDM-UHFFFAOYSA-N

物化性质

• 熔点：
  150-152℃
• 溶解度：
  溶于 DMSO（高达 25 mg/ml）。

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  70.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-溴-3-甲基丁醛 在 propylphosphonic anhydride 、 三乙胺 作用下， 以 乙醇 、 乙酸乙酯 为溶剂， 反应 18.0h， 生成 N-(5-异丙基-1,3-噻唑-2-基)-2-苯基乙酰胺
  参考文献：
  名称：

  Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease

  摘要：

  High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide (1). This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.09.006

文献信息

• GUT FLORA-DERIVED EXTRACELLULAR VESICLES, AND METHOD FOR SEARCHING FOR A DISEASE MODEL, VACCINE, AND CANDIDATE DRUG AND FOR DIAGNOSIS USING SAME
  申请人：Aeon Medix Inc.

  公开号：EP2494865A2

  公开（公告）日：2012-09-05

  The present invention relates to a composition including gut flora-derived extracellular vesicles, and to an animal disease model using same. In addition, the present invention relates to a method for using the gut flora-derived extracellular vesicles to efficiently search for a candidate drug which may prevent or treat diseases that occur due to gut flora-derived extracellular vesicles, and to a vaccine which can efficiently prevent or treat infections caused by gut flora or diseases that occur due to gut flora-derived extracellular vesicles. Further, the development of diagnostic technology to discover, using the gut flora-derived extracellular vesicles of the present invention, the etiology of diseases that occur due to gut flora-derived extracellular vesicles, can be achieved.

  本发明涉及一种包括源自肠道菌群的细胞外囊泡的组合物，以及使用该组合物的动物疾病模型。此外，本发明还涉及一种使用肠道菌群衍生的胞外囊泡来有效寻找候选药物的方法，该候选药物可预防或治疗因肠道菌群衍生的胞外囊泡而发生的疾病；本发明还涉及一种疫苗，该疫苗可有效预防或治疗由肠道菌群引起的感染或因肠道菌群衍生的胞外囊泡而发生的疾病。此外，还可以开发诊断技术，利用本发明的肠道菌群源性细胞外囊泡发现因肠道菌群源性细胞外囊泡引起的疾病的病因。
• 2-AMINO-THIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS ANTITUMOR AGENTS
  申请人：Pharmacia Italia S.p.A.

  公开号：EP1124810B9

  公开（公告）日：2005-12-28
• GUT FLORA-DERIVED EXTRACELLULAR VESICLES, AND METHOD FOR SEARCHING FOR A DISEASE MODEL, VACCINE, AND CANDIDATE DRUG AND FOR DIAGNOSIS USING THE SAME
  申请人：Kim Yoon Keun

  公开号：US20120222142A1

  公开（公告）日：2012-08-30

  The present application relates to a composition including gut flora-derived extracellular vesicles, and to an animal disease model using same. In addition, the present application relates to a method for using the gut flora-derived extracellular vesicles to efficiently search for a candidate drug which may prevent or treat diseases that occur due to gut flora-derived extracellular vesicles, and to a vaccine which can efficiently prevent or treat infections caused by gut flora or diseases that occur due to gut flora-derived extracellular vesicles. Further, the development of diagnostic technology to discover, using the gut flora-derived extracellular vesicles of the present application, the etiology of diseases that occur due to gut flora-derived extracellular vesicles, can be achieved.
• US7037929B1
  申请人：——

  公开号：US7037929B1

  公开（公告）日：2006-05-02
• US9201072B2
  申请人：——

  公开号：US9201072B2

  公开（公告）日：2015-12-01