2-<3-(3-pyridinyloxy)propyl>-1H-isoindole-1,3(2H)-dione | 122213-99-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 2-<3-(3-pyridinyloxy)propyl>-1H-isoindole-1,3(2H)-dione
• 英文别名: N-(3-(pyridin-3-yloxy)propyl)phthalimide；N-(3-(3-pyridyloxy)propyl)phthalimide；2-[3-(3-pyridinyloxy)propyl]-1H-isoindole-1,3(2H)-dione；2-(3-pyridin-3-yloxypropyl)isoindole-1,3-dione
• CAS: 122213-99-4
• 化学式: C₁₆H₁₄N₂O₃
• 分子量: 282.299
• InChiKey: AIGWHRFYHKLKQV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  59.5
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-<3-(3-pyridinyloxy)propyl>-1H-isoindole-1,3(2H)-dione 在 一水合肼 作用下， 以 乙醇 为溶剂， 以80%的产率得到3-(3-吡啶氧基)-1-丙胺
  参考文献：
  名称：

  Pentadienyl carboxamide derivatives as antagonists of platelet activating factor

  摘要：

  A series of N-[4-(3-pyridinyl)butyl]-5,5-disubstituted-pentadienamides was prepared and evaluated for PAF-antagonist activity. Compounds were assayed in vitro in a PAF-binding assay employing washed, whole dog platelets as the receptor source and in vivo after intravenous or oral administration for their ability to prevent PAF-induced bronchoconstriction in guinea pigs. Criteria required for good oral activity in the latter model include an (E,-E)-5-phenyl-2,4-pentadienamide, a second phenyl or a four- or five-carbon alkyl moiety in the 5-position of the diene, and an (R)-[1-alkyl-4-(3-pyridinyl)butyl] substituent on the carboxamide nitrogen atom. The alkyl substituent on this side chain can be methyl, ethyl, or cyclopropyl. Two members of this series, [R-(E)]-5,5-bis(4-methoxy-phenyl)-N- [1-methyl-4-(3-pyridinyl)butyl]- 2,4-pentadienamide (31) and [R-(E,E)]-5-(4-methoxyphenyl)-N-[1-methyl-4- (3-pyridinyl)butyl]-2,4-decadienamide (58), were selected for further pharmacological evaluation. Both were found to be substantially longer acting after oral administration than the corresponding S enantiomers in the guinea pig bronchoconstriction assay. A second in vivo model used to evaluate PAF antagonists determines the ability of test compounds to decrease the area of skin wheals induced by an intradermal injection of PAF. In this model, using both rats and guinea pigs, compounds 31 and 58 were found to be as active as the reference PAF antagonist 3-[4-(2-chlorophenyl)-9-methyl-6H- 1-(4-morpholinyl)-1-propanone (45).

  DOI：

  10.1021/jm00128a026
• 作为产物：
  描述：

  3-羟基吡啶 、 N-(3-溴丙基)苯二胺 在 NaH 作用下， 以 水 、 N,N-二甲基甲酰胺 为溶剂， 生成 2-<3-(3-pyridinyloxy)propyl>-1H-isoindole-1,3(2H)-dione
  参考文献：
  名称：

  3-descladinose-2,3-anhydroerythromycin derivatives

  摘要：

  小说3-去氧-2,3-脱氧麦迪霉素化合物及其具有抗菌活性的药用盐和酯。

  公开号：

  US05750510A1

文献信息

• Omega-[(hetero)alkyl]benz[cd]indol-2-amines
  申请人：AMERICAN CYANAMID COMPANY

  公开号：EP0230035A2

  公开（公告）日：1987-07-29

  Omega-[(hetero)alkyl]benz[cd]indol-2-amines useful in inhibition of thromboxane synthetase and in treatment of hypertension in warm-blooded animals are disclosed.

  公开了可用于抑制血栓素合成酶和治疗温血动物高血压的ω-[（杂）烷基]苯并[cd]吲哚-2-胺。
• GUTHRIE, ROBERT W.;KAPLAN, GERALD L.;MENNONA, FRANCIS A.;TILLEY, JEFFERSO+, J. MED. CHEM., 32,(1989) N, C. 1820-1835
  作者：GUTHRIE, ROBERT W.、KAPLAN, GERALD L.、MENNONA, FRANCIS A.、TILLEY, JEFFERSO+

  DOI：——

  日期：——
• 3-DESCLADINOSE-2,3-ANHYDROERYTHROMYCIN DERIVATIVES
  申请人：ABBOTT LABORATORIES

  公开号：EP0922050B1

  公开（公告）日：2003-07-30
• US5081131A
  申请人：——

  公开号：US5081131A

  公开（公告）日：1992-01-14
• US5750510A
  申请人：——

  公开号：US5750510A

  公开（公告）日：1998-05-12