5-<2-<4'-(acetoxymethyl)biphenylyl>>-2-(triphenylmethyl)-2H-tetrazole | 154709-17-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 5-<2-<4'-(acetoxymethyl)biphenylyl>>-2-(triphenylmethyl)-2H-tetrazole
• 英文别名: 4-(acetoxymethyl)-2'-(1-triphenylmethyltetrazol-5-yl)biphenyl；[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methyl acetate
• CAS: 154709-17-8
• 化学式: C₃₅H₂₈N₄O₂
• 分子量: 536.633
• InChiKey: DQQWYTLRFNCRSF-UHFFFAOYSA-N

物化性质

• 沸点：
  719.2±70.0 °C(Predicted)
• 密度：
  1.17±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  7.3
• 重原子数：
  41
• 可旋转键数：
  9
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  69.9
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-<2-<4'-(acetoxymethyl)biphenylyl>>-2-(triphenylmethyl)-2H-tetrazole 在 LiAlH4 作用下， 以 四氢呋喃 、 水 为溶剂， 以83%的产率得到5-[4’-羟基甲基-(1,1’-联苯)-2-基]-2-三苯基甲基四唑
  参考文献：
  名称：

  Imidazole derivatives having a II antagonist activity

  摘要：

  咪唑衍生物具有A II拮抗活性，具有公式I的化合物，其制备方法，含有它们的药物组合物以及将其用作治疗剂的用途。具有A II拮抗活性的描述化合物可用于各种心血管疾病。

  公开号：

  US05587390A1
• 作为产物：
  描述：

  potassium acetate 、 N-(三苯基甲基)-5-(4'-溴甲基联苯-2-基)四氮唑 在 18-冠醚-6 作用下， 以 乙二醇二甲醚 为溶剂， 反应 20.0h， 以87%的产率得到5-<2-<4'-(acetoxymethyl)biphenylyl>>-2-(triphenylmethyl)-2H-tetrazole
  参考文献：
  名称：

  New nonpeptide angiotensin II receptor antagonists. 2. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)quinoline derivatives

  摘要：

  A novel series of nonpeptidic angiotensin II (AII) receptor antagonists is reported, derived from linkage of the biphenylcarboxylic acid or biphenylyltetrazole moiety found in previously described antagonists via a methyleneoxy chain to the 4-position of a 2-alkyl quinoline. When evaluated in an in vitro binding assay using a guinea pig adrenal membrane preparation, compounds in this series generally gave IC50 values in the range 0.01-1 muM. Structure-activity studies showed the quinoline nitrogen atom and a short alkyl chain at the quinoline 2-position to be essential for receptor binding. On intravenous administration in a normotensive rat model, the more potent compounds inhibited the AII-induced pressor response with ED50 values in the range 0.1-2.0 mg/kg. One of the compounds, 2-ethyl-4-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methoxy]quinoline (5g), demonstrated good oral activity in two rat models. At doses in the range 1-10 mg/kg in AII-infused, normotensive rats, the compound exhibited a dose-related inhibition of the pressor response with a good duration of action at the higher doses. In a renal hypertensive rat model, compound 5g showed a rapid and sustained lowering of blood pressure at a dose of 5 mg/kg. On the basis of its profile, this compound, designated ICID8731, has been selected for clinical evaluation.

  DOI：

  10.1021/jm00100a007

文献信息

• IMIDAZOLE DERIVATIVES HAVING ANGIOTENSIN II ANTAGONIST ACTIVITY
  申请人：ISTITUTO LUSO FARMACO D'ITALIA S.p.A.

  公开号：EP0654030B1

  公开（公告）日：1996-12-18
• US5587390A
  申请人：——

  公开号：US5587390A

  公开（公告）日：1996-12-24
• [EN] IMIDAZOLE DERIVATIVES HAVING A II ANTAGONIST ACTIVITY<br/>[FR] DERIVES D'IMIDAZOLE A ACTIVITE ANTAGONISTE DE L'ANGIOTENSINE II
  申请人：ISTITUTO LUSO FARMACO D'ITALIA S.P.A.

  公开号：WO1994003449A1

  公开（公告）日：1994-02-17

  (EN) Imidazole derivatives having A II antagonist activity, of formula (I), the processes for the preparation thereof, pharmaceutical compositions containing them and the use thereof as therapeutical agents. The described compounds have A II antagonist activity and they can be used in various cardiovascular disorders.(FR) Dérivés d'imidazole présentant une activité antagoniste de l'angiotensine II, de la formule (I), leurs procédés de préparation, compositions pharmaceutiques les contenant et leur utilisation comme agents thérapeutiques. Les composés de l'invention présentent une activité antagoniste de l'angiotensine II et on peut les utiliser dans le traitement de divers troubles cardiovasculaires.