2-(4-Methylpiperazino)-4-phenyl-6-chlor-chinolin | 31576-85-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 2-(4-Methylpiperazino)-4-phenyl-6-chlor-chinolin
• 英文别名: 6-chloro-2-(4-methyl-piperazin-1-yl)-4-phenyl-quinoline；6-Chloro-2-(4-methylpiperazin-1-yl)-4-phenylquinoline
• CAS: 31576-85-9
• 化学式: C₂₀H₂₀ClN₃
• 分子量: 337.852
• InChiKey: PTRMVVJMLDKZBI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  24
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  19.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  6-Chloro-2-(4-methylpiperazin-1-yl)-4-phenylquinoline;dihydrochloride 生成 2-(4-Methylpiperazino)-4-phenyl-6-chlor-chinolin
  参考文献：
  名称：

  HINO KATSUHIKO; FURUKAWA KIYOSHI; NAGAI YASUTAKA; UNO HITOSHI, CHEM. AND PHARM. BULL., 1980, 28, NO 9, 2618-2622

  摘要：

  DOI：

文献信息

• 4-Phenyl-2-(1-piperazinyl)quinolines with potent antidepressant activity.
  作者：KATSUHIKO HINO、KIYOSHI FURUKAWA、YASUTAKA NAGAI、HITOSHI UNO

  DOI：10.1248/cpb.28.2618

  日期：——

  A series of 2-amino-4-phenylquinolines was synthesized and the effects of these compounds on the central nervous system were evaluated pharmacologically in mice. Among these compounds, many 2-(substituted piperazinyl) derivatives exhibited a potent antagonism to hypothermia and catalepsy induced by reserpine, as well as some inhibitory effect on locomotor activity. Some compounds were found to possess activity to inhibit tremorine-induced tremor.

  合成了一系列2-氨基-4-苯基喹啉，并在小鼠中药理评估了这些化合物对中枢神经系统的影响。在这些化合物中，许多2-(取代哌嗪基)衍生物表现出对美克洛西丁诱导的低体温和植物人状态的显著拮抗作用，同时对运动活动也有一定的抑制效果。一些化合物被发现具有抑制颤动素诱发的震颤的活性。
• Anti-peptic ulcer agent
  申请人：Dainippon Pharmaceutical Co., Ltd.

  公开号：EP0127189A2

  公开（公告）日：1984-12-05

  Use of 2-(4-ethyl-1-piperazinyl)-4-phenylquinoline or a pharmaceutically acceptable saltthereoffor prophylaxis and/or treatment of peptic ulcer, and a method for prophylaxis and/or treatment of peptic ulcer disease which comprises administering an effective amount of the above-mentioned compound to warm blood animal, especially human. Said active compounds have excellent pharmacological activities such as inhibition of ulceration and inhibition of gastric secretion, and hence, are useful as an anti-peptic ulcer agent.

  2-(4-乙基-1-哌嗪基)-4-苯基喹啉或其药学上可接受的盐用于预防和/或治疗消化性溃疡的用途，以及一种预防和/或治疗消化性溃疡病的方法，该方法包括向温血动物，特别是人，施用有效量的上述化合物。上述活性化合物具有良好的药理活性，如抑制溃疡和抑制胃液分泌，因此可用作抗消化性溃疡剂。
• 2-(1-PIPERAZINYL)-4-SUBSTITUTED PHENYLQUINOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND MEDICINAL COMPOSITION CONTAINING SAME
  申请人：Dainippon Pharmaceutical Co., Ltd.

  公开号：EP0204003A1

  公开（公告）日：1986-12-10

  Compounds represented by the general formula (1), (wherein R1 represents a fluorine atom in p-position, a chlorine atom in p-position, a methyl group in p-position or a trifluoromethyl group in p- or m-position, and R2 represents a hydrogen atom, a methyl group, an ethyl group, a 2-hydroxyethyl group or a 3-hydroxypropyl group, provided that R2 represents an ethyl group, a 2-hydroxyethyl group or a 3-hydroxypropyl group when R, represents a fluorine atom in p-position, a methyl group in p-position or a trifluoromethyl group in p-position), physiologically acceptable salts thereof, process for their preparation, and medicinal composition. These compounds and salts possess an excellent mucous membrane-protecting effect, and are useful for prophylaxis and treatment of peptic ulcer and inflammatory diseases of gastrointestinal tracts.

  通式(1)所代表的化合物，（其中 R1 代表 p 位的氟原子、p 位的氯原子、p 位的甲基或 p 位或 m 位的三氟甲基，R2 代表氢原子、甲基、乙基、2-羟乙基或 3-羟丙基、当 R 代表 p 位的氟原子、p 位的甲基或 p 位的三氟甲基时，R2 代表乙基、2-羟乙基或 3-羟丙基）、其生理上可接受的盐、其制备方法和药物组合物。这些化合物和盐具有良好的粘膜保护作用，可用于预防和治疗消化性溃疡和胃肠道炎症性疾病。
• US4237135A
  申请人：——

  公开号：US4237135A

  公开（公告）日：1980-12-02
• US4677107A
  申请人：——

  公开号：US4677107A

  公开（公告）日：1987-06-30