3-Hydroxy-7,8-dimethoxy-1-methylisoquinoline | 34140-44-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: 3-Hydroxy-7,8-dimethoxy-1-methylisoquinoline
• 英文别名: 6,7-Dimethoxy-3-isoquinolinol；6,7-dimethoxy-2H-isoquinolin-3-one
• CAS: 34140-44-8
• 化学式: C₁₁H₁₁NO₃
• 分子量: 205.213
• InChiKey: ABGRUHODZWXRCB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  47.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-Hydroxy-7,8-dimethoxy-1-methylisoquinoline 在 硝酸 、 溶剂黄146 作用下， 以 吡啶 为溶剂， 反应 0.5h， 生成 6,7-dimethoxy-4-nitro-3-(trifluoromethanesulfonyloxy)isoquinoline
  参考文献：
  名称：

  Singh, Sudhir K.; Ruchelman, Alexander L.; Zhou, Nai, Medicinal Chemistry Research, 2003, vol. 12, # 1, p. 1 - 12

  摘要：

  DOI：

文献信息

• Renal vasodilators. The role of the 4-substituent in isoquinolin-3-ol cardiovascular agents. 4-Ureido derivatives of isoquinolin-3-ol with selective renal vasodilator properties
  作者：Ramesh M. Kanojia、O. William Lever、Jeffery B. Press、Louella Williams、Harvey M. Werblood、Edward C. Giardino、Robert Falotico、Alfonso J. Tobia

  DOI：10.1021/jm00125a011

  日期：1989.5

  The synthesis and cardiovascular evaluation of a series of isoquinolin-3-ol derivatives bearing a variety of nitrogen substituents (amino, acylamino, carbamate, and ureido) at C-4 are described. Certain of these compounds have a selective renal vasodilating profile and have minimal effects on arterial blood pressure or heart rate when administered intravenously in the instrumented anesthetized dog

  描述了一系列在C-4带有多个氮取代基（氨基，酰基氨基，氨基甲酸酯和脲基）的异喹啉-3-醇衍生物的合成及心血管系统评价。这些化合物中的某些具有选择性的肾血管舒张特性，并且在用仪器麻醉的狗中静脉内给药时对动脉血压或心率的影响最小。该系列中最有效的肾血管舒张药是4-（烯丙基铝）-6,7-二甲氧基异喹啉-3-醇（38），以1.2 mg / kg的剂量静脉注射可使肾血流量最大增加97％，而无明显变化降压或变时作用。讨论了有关异喹啉醇核芳香环中4-取代基的性质和烷氧基取代模式的结构活性观察结果。
• Isoquinolinol derivatives: potent, short-acting inotropic and vasodilating agents with potential utility for cardiac emergencies
  作者：RM Kanojia、JB Press、OW Lever、L Williams、HM Werblood、R Falotico、JM Moore、AJ Tobia

  DOI：10.1016/0223-5234(91)90023-g

  日期：1991.3

  The synthesis and cardiovascular evaluation of a series of 4-nitroisoquinolin-3-ol derivatives are reported. These compounds are potent, short-acting cardiovascular agents with both positive inotropic and peripheral vasodilating effects when administered intravenously. Compounds with this profile could be of particular therapeutic benefit in cardiac emergencies such as severe late stage heart failure and myocardial infarction. Of particular interest is 7-ethoxy-6-methoxy-1-methyl-4-nitroisoquinolin-3-ol (6) which has potent, non beta-adrenergic parenteral inotropic properties similar to those of dopamine, and also has peripheral vasodilator activity, up to 10-fold greater than amrinone.
• INDAZOLE DERIVATIVES AS JNK INHIBITORS
  申请人：SIGNAL PHARMACEUTICALS, INC.

  公开号：EP1313711A2

  公开（公告）日：2003-05-28
• EP1618093A2
  申请人：——

  公开号：EP1618093A2

  公开（公告）日：2006-01-25
• [EN] INDAZOLE DERIVATIVES AS JNK INHIBITORS AND COMPOSITIONS AND METHODS RELATED THERETO<br/>[FR] DERIVES D'INDAZOLE UTILISES COMME INHIBITEURS DE JNK ET COMPOSITIONS ET METHODES ASSOCIEES A CEUX-CI
  申请人：SIGNAL PHARM INC

  公开号：WO2002010137A2

  公开（公告）日：2002-02-07

  Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: (I), wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.