4,5-dihydro-5-methyl-6-(2-methylamino-4-propylamino-7-quinazolinyl)-3(2H)-pyridazinone | 124294-71-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 4,5-dihydro-5-methyl-6-(2-methylamino-4-propylamino-7-quinazolinyl)-3(2H)-pyridazinone
• 英文别名: 4,5-dihydro-5-methyl-6-(2-methylamino-4-n-propylaminoquinazolin-7-yl)-3(2H)-pyridazinone；4-methyl-3-[2-(methylamino)-4-(propylamino)quinazolin-7-yl]-4,5-dihydro-1H-pyridazin-6-one
• CAS: 124294-71-9
• 化学式: C₁₇H₂₂N₆O
• 分子量: 326.401
• InChiKey: JWHSGXBEPXSTKB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  24
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  91.3
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  4,5-dihydro-6-(2,4-bismethylthio-7-quinazolinyl)-5-methyl-3(2H)-pyridazinone 在 potassium permanganate 作用下， 以 甲醇 为溶剂， 反应 10.67h， 生成 4,5-dihydro-5-methyl-6-(2-methylamino-4-propylamino-7-quinazolinyl)-3(2H)-pyridazinone
  参考文献：
  名称：

  Studies on cardiotonic agents. VII. Potent cardiotonic agent KF15232 with myofibrillar Ca2+ sensitizing effect.

  摘要：

  一系列新型的4,5-二氢-5-甲基-6-(2或4-取代的7-喹唑啉基)-3(2H)-哒嗪酮被合成并在麻醉犬中检测其强心活性。4-取代的氨基喹唑啉通常显示出强力且持久的正性肌力活性。当在喹唑啉环的2-位引入取代基时，活性下降。3-取代的4(3H)-喹唑啉亚胺通常显示出较弱的活性。4-取代氨基衍生物的钙离子增敏效应也在来自豚鼠乳头肌的化学剥离纤维中进行了研究。烷基氨基衍生物显示出小的增敏效应，而苄基氨基衍生物显示出较大的效应。其中，KF15232 (Ix) 被发现具有最强大的强心和钙离子增敏活性。

  DOI：

  10.1248/cpb.39.900

文献信息

• Quinazoline-substituted pyridazinone derivatives having cardiotonic
  申请人：Kyowa Hakko Kogyo Co., Ltd.

  公开号：US05063227A1

  公开（公告）日：1991-11-05

  Compounds of the formula ##STR1## wherein R.sub.3 is H or alkyl, Q.sub.1 and Q.sub.2 are independently hydrogen, alkyl, hydroxyl, alkoxyl, amino, mono or di alkylamino, nitro or halo or pharmaceutically acceptable salts are useful as cardiotonics.

  式为##STR1##的化合物，其中R.sub.3为H或烷基，Q.sub.1和Q.sub.2分别为氢、烷基、羟基、烷氧基、氨基、单烷基氨基、双烷基氨基、硝基或卤素，或其药学上可接受的盐，可用作心力补充剂。
• Novel pyridazinone derivatives and pharmaceutical preparations containing them
  申请人：KYOWA HAKKO KOGYO CO., LTD.

  公开号：EP0326307A2

  公开（公告）日：1989-08-02

  Novel pyridazinone compounds having cardiotonic activity are disclosed, being compounds represented by the following formula; and their pharmaceutically acceptable acid addition salts.

  本发明公开了具有强心活性的新型哒嗪酮化合物，即由下式表示的化合物； 及其药学上可接受的酸加成盐。
• US5063227A
  申请人：——

  公开号：US5063227A

  公开（公告）日：1991-11-05
• Studies on cardiotonic agents. VII. Potent cardiotonic agent KF15232 with myofibrillar Ca2+ sensitizing effect.
  作者：Yuji NOMOTO、Haruki TAKAI、Tetsuji OHNO、Kazuhiro KUBO

  DOI：10.1248/cpb.39.900

  日期：——

  A series of novel 4, 5-dihydro-5-methyl-6-(2 or 4-substituted 7-quinazolinyl)-3(2H)-pyridazinones was synthesized and examined for cardiotonic activity in anesthetized dogs. The 4-substituted aminoquinazolines generally showed potent and long-lasting inotropic activity. Fall in the activity was observed on the introduction of substituent at the 2-position of the quinazoline ring. The 3-substituted 4 (3H)-quinazolinimines generally exhibited weak activity. Ca+2 sensitizing effect of the 4-substituted amino derivatives was also examined in chemically skinned fiber from papillary muscle of guinea pig. The alkylamino derivatives exhibited small sensitizing effect, while the benzylamino derivatives exhibited large effect. Among them, KF15232 (Ix) was found to have the most potent cardiotonic and Ca2+ sensitizing activities.

  一系列新型的4,5-二氢-5-甲基-6-(2或4-取代的7-喹唑啉基)-3(2H)-哒嗪酮被合成并在麻醉犬中检测其强心活性。4-取代的氨基喹唑啉通常显示出强力且持久的正性肌力活性。当在喹唑啉环的2-位引入取代基时，活性下降。3-取代的4(3H)-喹唑啉亚胺通常显示出较弱的活性。4-取代氨基衍生物的钙离子增敏效应也在来自豚鼠乳头肌的化学剥离纤维中进行了研究。烷基氨基衍生物显示出小的增敏效应，而苄基氨基衍生物显示出较大的效应。其中，KF15232 (Ix) 被发现具有最强大的强心和钙离子增敏活性。