2-Methyl-N-[4-[(5(6H)-phenanthridinyl)carbonyl]-phenyl]benzamide

• 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: 2-Methyl-N-[4-[(5(6H)-phenanthridinyl)carbonyl]-phenyl]benzamide
• 英文别名: 2-Methyl-N-[4-[(5(6H)-phenanthridinyl)carbonyl]phenyl]benzamide；2-methyl-N-[4-(6H-phenanthridine-5-carbonyl)phenyl]benzamide
• 化学式: C₂₈H₂₂N₂O₂
• 分子量: 418.495
• InChiKey: AROSNMSHTYIBMN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  32
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  49.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  6(5H)-菲啶酮 在 dimethyl sulfide borane 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 生成 2-Methyl-N-[4-[(5(6H)-phenanthridinyl)carbonyl]-phenyl]benzamide
  参考文献：
  名称：

  Structure–activity study of novel tricyclic benzazepine arginine vasopressin antagonists

  摘要：

  Novel tricyclic benzazepine derivatives were synthesized as arginine vasopressin (AVP) antagonists. Several tricyclic compounds showed potent antagonistic activity in rat AVP receptors V-1a and V-2. Derivatives containing pyrrolo-tricyclic amines, 13i-k. 30, and 31 also showed selectivity for the V-2 receptor. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00388-3

文献信息

• Tricyclic benzazepine vasopressin antagonists
  申请人：American Cyanamid Company

  公开号：US05512563A1

  公开（公告）日：1996-04-30

  Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

  通用式I的三环化合物：##STR1##，如本文所定义，在V.sub.1和/或V.sub.2受体表现出拮抗活性，并在体内表现出抗利尿素拮抗活性，使用这种化合物治疗由肾脏过度重吸水而表现出的疾病的方法，以及制备这种化合物的方法。
• Tricyclic Benzazepine vasopressin antagonists
  申请人：American Cyanamid Company

  公开号：US05736538A1

  公开（公告）日：1998-04-07

  Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

  通用式I的三环化合物：##STR1##，如本文所定义，在V.sub.1和/或V.sub.2受体上表现出拮抗活性，并在体内表现出抗利尿素拮抗活性，使用这种化合物治疗由肾脏过度重吸水引起的疾病的方法，以及制备这种化合物的方法。
• Pyridobenzoxazepine and pyridobenzothiazepine vasopressin antagonists
  申请人：American Cyanamid Company

  公开号：US05686445A1

  公开（公告）日：1997-11-11

  Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

  一般式I的三环化合物：##STR1##在此定义下，表现出对V.sub.1和/或V.sub.2受体的拮抗活性，并在体内表现出抗利尿激素拮抗活性。本发明提供使用此类化合物治疗由肾水过度重吸收所特征的疾病的方法，并提供制备此类化合物的方法。
• N-acylated tricyclic azaheterorings useful as vasopressin antagonists
  申请人：American Cyanamid Company

  公开号：EP0640592B1

  公开（公告）日：1998-12-30
• Structure–activity study of novel tricyclic benzazepine arginine vasopressin antagonists
  作者：Fuk-Wah Sum、John Dusza、Efren Delos Santos、George Grosu、Marvin Reich、Xumei Du、J.Donald Albright、Peter Chan、Joseph Coupet、Xun Ru、Hossein Mazandarani、Trina Saunders

  DOI：10.1016/s0960-894x(03)00388-3

  日期：2003.7

  Novel tricyclic benzazepine derivatives were synthesized as arginine vasopressin (AVP) antagonists. Several tricyclic compounds showed potent antagonistic activity in rat AVP receptors V-1a and V-2. Derivatives containing pyrrolo-tricyclic amines, 13i-k. 30, and 31 also showed selectivity for the V-2 receptor. (C) 2003 Elsevier Science Ltd. All rights reserved.