phthalimidyl imidazole | 185563-91-1

• 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: phthalimidyl imidazole
• 英文别名: 2-Phthalimidoimidazole；Phthalimidoimidazole；2-(1H-imidazol-2-yl)isoindole-1,3-dione
• CAS: 185563-91-1
• 化学式: C₁₁H₇N₃O₂
• 分子量: 213.195
• InChiKey: NIMMZHAMBMAFEG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  66.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  三苯基氯甲烷 、 phthalimidyl imidazole 在 吡啶 作用下， 反应 24.0h， 以27.5%的产率得到1Triphenylmethyl-2-phthalimidoimidazole
  参考文献：
  名称：

  Isoxazolines as Potent Antagonists of the Integrin α_vβ₃

  摘要：

  Starting with lead compound 2, we sought to increase the selectivity for alpha(v)beta(3)-mediated cell adhesion by examining the effects of structural changes in both the guanidine mimetic and the substituent alpha to the carboxylate. To prepare some of the desired aminoimidazoles, a novel reductive amination utilizing a trityl-protected aminoimidazole was developed. It was found that guanidine mimetics with a wide range of pK(a)'s were potent antagonists of alpha(v)beta(3). In general, it appeared that an acylated 2-aminoimidazole guanidine mimetic imparted excellent selectivity for alpha(v)beta(3)-mediated adhesion versus alpha(IIb)beta(3)-mediated platelet aggregation, with selectivity of approximately 3 orders of magnitude observed for compounds 3g and 3h. It was also found in this series that the alpha-substituent was required for potent activity and that 2,6-disubstituted arylsulfonamides were optimal. In addition, the selective alpha(v)beta(3) antagonist 3h was found to be a potent inhibitor of alpha(v)beta(3)-mediated cell migration.

  DOI：

  10.1021/jm9900321
• 作为产物：
  描述：

  苯酐 生成 phthalimidyl imidazole
  参考文献：
  名称：

  Integrin receptor antagonists

  摘要：

  这项发明涉及新颖的杂环化合物，包括3-\x9b1-\x9b3-(咪唑啉-2-基氨基)丙基!吲唑-5-基甲酰胺!-2-(苄氧羰基氨基)丙酸，这些化合物可作为α.sub.v β.sub.3整合素及相关细胞表面粘附蛋白受体的拮抗剂，用于含有这些化合物的药物组合物，制备这些化合物的方法，以及使用这些化合物单独或与其他治疗剂联合用于抑制细胞黏附、治疗血管生成障碍、炎症、骨质疏松、癌症转移、糖尿病性视网膜病变、血栓形成、再狭窄、黄斑变性以及其他由细胞黏附和/或细胞迁移和/或血管生成介导的疾病的方法。

  公开号：

  US05760028A1

文献信息

• Nucleosidic and non-nucleosidic folate conjugates
  申请人：ISIS Pharmaceuticals, Inc.

  公开号：US20020049163A1

  公开（公告）日：2002-04-25

  Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2′-, 3′-, 5′-, nucleobase and internucleotide linkage sites. The folate can be attached via the &agr;- or &ggr;-carboxylate, optionally through a linking group. Methods for the regiospecific synthesis of the conjugates are diclosed. Also disclosed are nucleosidic and non-nucleosidic linkers conjugated to folic acid and related folates.

  描述了寡核苷酸-叶酸共轭物，其中叶酸与寡核苷酸的2'-、3'-、5'-、核碱基和核苷酸间连接位点之一或多个位点结合。叶酸可以通过α-或γ-羧酸酯连接，可选地通过连接基团连接。公开了合成共轭物的区域特异性方法。还公开了与叶酸及相关叶酸共轭的核苷酸和非核苷酸连接剂。
• Novel (aryl or heteroaromatic methyl)-2,2'-BI-1H-imidazoles
  申请人：MERRELL DOW PHARMACEUTICALS INC.

  公开号：EP0301456A2

  公开（公告）日：1989-02-01

  This invention relates to novel (aryl or heteroaromatic methyl)-2,2′-1H-biimidazoles; to a process for their production comprising of reacting an appropriate alpha-brominated or alpha-chlorinated, substituted or non-­substituted, methylated monoaromatic ring compound with 2,2′-bi-1H-imidazole in a solvent such as ethanol in the presence of a base such as sodium hydroxide under reflux conditions; and to pharmaceutical compositions and methods of treating hypertension with such compounds.

  本发明涉及新型（芳基或杂芳甲基）-2,2′-1H-咪唑；涉及其生产工艺，包括在回流条件下，在乙醇等溶剂中，在氢氧化钠等碱存在下，使适当的α-溴化或α-氯化、取代或非取代、甲基化的单芳香环化合物与2,2′-1H-咪唑反应；以及用这种化合物治疗高血压的药物组合物和方法。
• US4929744A
  申请人：——

  公开号：US4929744A

  公开（公告）日：1990-05-29
• US5426105A
  申请人：——

  公开号：US5426105A

  公开（公告）日：1995-06-20
• US5674879A
  申请人：——

  公开号：US5674879A

  公开（公告）日：1997-10-07