2-hydroxy-N'-[2-(2-naphthyloxy)acetyl]benzohydrazide

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 2-hydroxy-N'-[2-(2-naphthyloxy)acetyl]benzohydrazide
• 英文别名: 2-hydroxy-N'-(2-naphthalen-2-yloxyacetyl)benzohydrazide
• 化学式: C₁₉H₁₆N₂O₄
• 分子量: 336.347
• InChiKey: YXWKZOKDIMSTRT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  87.7
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-(2-萘氧基)乙酰肼 、 水杨酰氯 在 4-乙烯基吡啶 作用下， 以 四氢呋喃 为溶剂， 以86%的产率得到2-hydroxy-N'-[2-(2-naphthyloxy)acetyl]benzohydrazide
  参考文献：
  名称：

  酰胺高速模拟的协议。新型小分子组织蛋白酶D抑制剂的制备

  摘要：

  已经建立了使用聚合物结合的试剂通过酰基氯，磺酰氯和羧酸与氮亲核试剂偶联来溶液相平行合成新的小分子组织蛋白酶D抑制剂的程序，以促进化学反应和/或有效清除未反应的起始物。材料和反应副产物。苯甲酸银（I）用于促进酰氯与反应性较小的苯胺的偶联。化合物4被鉴定为亚微摩尔组织蛋白酶D抑制剂（IC 50 = 320 nM）。

  DOI：

  10.1016/s0040-4039(99)01972-3

文献信息

• NOVEL COMPOUNDS FOR TREATMENT OF CANCER AND DISORDERS ASSOCIATED WITH ANGIOGENESIS FUNCTION
  申请人：Neamati Nouri

  公开号：US20090093489A1

  公开（公告）日：2009-04-09

  Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression.

  新型化合物用于治疗癌症和与血管生成功能相关的疾病。还公开了制备这些化合物的方法、含有这些化合物的药物组合物和包装产品、使用这些分子治疗癌症（例如白血病、非小细胞肺癌、结肠癌、中枢神经系统癌症、黑色素瘤、卵巢癌、乳腺癌、肾癌和前列腺癌）和与血管生成功能相关的疾病（例如年龄相关性黄斑变性、黄斑营养不良和糖尿病）的方法、监测治疗的方法、基因表达谱分析的方法以及调节细胞生长、细胞周期、细胞凋亡或基因表达的方法。
• Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function
  申请人：Neamati Nouri

  公开号：US20100120781A1

  公开（公告）日：2010-05-13

  Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression.

  该专利涉及新型化合物，用于治疗癌症和与血管生成功能相关的疾病。还公开了制备这些化合物的方法，含有这些化合物的药物组合物和包装产品，使用这些分子治疗癌症（例如白血病、非小细胞肺癌、结肠癌、中枢神经系统癌症、黑色素瘤、卵巢癌、乳腺癌、肾癌和前列腺癌）和与血管生成功能相关的疾病（例如年龄相关性黄斑变性、黄斑营养不良和糖尿病）的方法，监测治疗的方法，基因表达谱分析的方法，以及细胞生长、细胞周期、凋亡或基因表达的调节方法。
• Novel Compounds for Treatment of Cancer and Disorders Associated With Angiogenesis Function
  申请人：NEAMATI Nouri

  公开号：US20110034472A1

  公开（公告）日：2011-02-10

  Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression.

  新型化合物用于治疗癌症和与血管生成功能相关的疾病。还公开了制备这些化合物的方法，含有这些化合物的药物组合物和包装产品，使用这些分子治疗癌症（例如白血病、非小细胞肺癌、结肠癌、中枢神经系统癌症、黑色素瘤、卵巢癌、乳腺癌、肾癌和前列腺癌）和与血管生成功能相关的疾病（例如年龄相关性黄斑变性、黄斑营养不良和糖尿病）的方法，监测治疗的方法，基因表达谱分析的方法，以及调节细胞生长、细胞周期、凋亡或基因表达的方法。
• Protocols for amide high-speed analoging. Preparation of novel, small molecule cathepsin D inhibitors
  作者：Jinshan Chen、Brian R. Dixon、Jacques Dumas、David Brittelli

  DOI：10.1016/s0040-4039(99)01972-3

  日期：1999.12

  Procedures for solution phase parallel synthesis of new, small molecule cathepsin D inhibitors by the coupling of acyl chlorides, sulfonyl chlorides and carboxylic acids with nitrogen nucleophiles have been established using polymer-bound reagents to facilitate the chemistry and/or to efficiently scavenge the unreacted starting materials and reaction by-products. Silver(I) benzoate was used to facilitate

  已经建立了使用聚合物结合的试剂通过酰基氯，磺酰氯和羧酸与氮亲核试剂偶联来溶液相平行合成新的小分子组织蛋白酶D抑制剂的程序，以促进化学反应和/或有效清除未反应的起始物。材料和反应副产物。苯甲酸银（I）用于促进酰氯与反应性较小的苯胺的偶联。化合物4被鉴定为亚微摩尔组织蛋白酶D抑制剂（IC 50 = 320 nM）。