N-[(2-methylphenyl)methyl]-6-pyridin-2-ylpyridazine-3-carboxamide | 1338225-38-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: N-[(2-methylphenyl)methyl]-6-pyridin-2-ylpyridazine-3-carboxamide
• CAS: 1338225-38-9
• 化学式: C₁₈H₁₆N₄O
• 分子量: 304.351
• InChiKey: PUHIOJQQQQTCOF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  67.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  6-氯哒嗪-3-甲酸甲酯 在 tris-(dibenzylideneacetone)dipalladium(0) 、 copper diacetate 、 potassium carbonate 、 2-二环己基磷-2,4,6-三异丙基联苯 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 生成 N-[(2-methylphenyl)methyl]-6-pyridin-2-ylpyridazine-3-carboxamide
  参考文献：
  名称：

  Structure–activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators

  摘要：

  Excitatory amino acid transporter 2 (EAAT2) is the major glutamate transporter and functions to remove glutamate from synapses. A thiopyridazine derivative has been found to increase EAAT2 protein levels in astrocytes. A structure-activity relationship study revealed that several components of the molecule were required for activity, such as the thioether and pyridazine. Modification of the benzylthioether resulted in several derivatives (7-13, 7-15 and 7-17) that enhanced EAAT2 levels by >6-fold at concentrations <5 mu M after 24 h. In addition, one of the derivatives (7-22) enhanced EAAT2 levels 3.5-3.9-fold after 24 h with an EC50 of 0.5 mu M. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.08.009

文献信息

• [EN] PYRIDAZINE DERIVATIVES AS EAAT2 ACTIVATORS<br/>[FR] DÉRIVÉS DE PYRIDAZINE EN TANT QU'ACTIVATEURS D'EAAT2
  申请人：BRIGHAM & WOMENS HOSPITAL

  公开号：WO2013019938A1

  公开（公告）日：2013-02-07

  Pyridazine derivatives that activate the excitatory amino acid transporter 2 (EAAT2), and methods of use thereof for treating or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.

  吡啶二氮杂苯衍生物可激活兴奋性氨基酸转运蛋白2（EAAT2），以及利用这些方法治疗或预防与谷氨酸兴奋毒性相关的疾病、障碍和症状。
• US9447075B2
  申请人：——

  公开号：US9447075B2

  公开（公告）日：2016-09-20