1-(3-chloropropyl)-7-methoxy-1H-indole | 944086-42-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1-(3-chloropropyl)-7-methoxy-1H-indole
• 英文别名: 1-(3-chloropropyl)-7-methoxyindole
• CAS: 944086-42-4
• 化学式: C₁₂H₁₄ClNO
• 分子量: 223.702
• InChiKey: GUDUZPKJIBCLLG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  14.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  1-(3-chloropropyl)-7-methoxy-1H-indole 、 3,4-二氯苄基异氰酸酯 在 magnesium iodide 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 2.0h， 生成 1-(3-chloropropyl)-N-(3,4-dichlorobenzyl)-7-methoxy-1H-indole-3-carboxamide
  参考文献：
  名称：

  WO2007/79239

  摘要：

  公开号：
• 作为产物：
  描述：

  7-甲氧基吲哚 、 1-溴-3-氯丙烷 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 0.33h， 以58%的产率得到1-(3-chloropropyl)-7-methoxy-1H-indole
  参考文献：
  名称：

  Indolylalkyltriphenylphosphonium Analogues Are Membrane-Depolarizing Mycobactericidal Agents

  摘要：

  Agents that selectively target the mycobacterial membrane could potentially shorten treatment time for tuberculosis, reduce relapse, and curtail emergence of resistant strains. The lipophilicity and extensive charge-delocalized state of the triphenylphosphonium cation strongly favor accumulation within bacterial membranes. Here, we explored the antimycobacterial activities and membrane-targeting properties of indolylalkyltriphenylphosphonium analogues. The most active analogues preferentially inhibited growth of Mycobacterium tuberculosis H37Rv (MIC50 2-4 mu M) and were bactericidal against Mycobacterium bovis BCG (MBC99 3 mu M). In spite of their propensity to accumulate within membranes, we found no evidence that these compounds permeabilized mycobacterial membranes or induced cell-envelope stress. Our investigations indicated that their bacterical effects stem from sustained depolarization of mycobacterial membranes and ensuing disruptive effects on electron transfer and cell division.

  DOI：

  10.1021/acsmedchemlett.7b00287

文献信息

• BICYCLIC-NITROGEN COMPOUNDS AS MODULATORS OF GHRELIN RECEPTOR AND USES THEREOF
  申请人：Burstein S. Ethan

  公开号：US20070213359A1

  公开（公告）日：2007-09-13

  Disclosed herein are compounds of Formula I as defined herein, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, that modulates the activity of a ghrelin receptor. Disclosed herein are also methods of treating diseases or conditions that comprise administering to a subject in need thereof a therapeutically effective amount of a compound of Formula I.

  本文披露了一些公式I定义的化合物，或其药学上可接受的盐，酯，酰胺或前药，该化合物调节胃饥饿素受体的活性。本文还披露了治疗疾病或病症的方法，包括向需要的受试者施用公式I的化合物的治疗有效量。
• [EN] BICYCLIC NITROGEN COMPOUNDS AS MODULATORS OF GHRELIN RECEPTOR AND USES THEREOF<br/>[FR] COMPOSES BICYCLIQUES A BASE D'AZOTE EN TANT QUE MODULATEURS DE RECEPTEUR DE GHRELINE ET LEURS UTILISATIONS
  申请人：ACADIA PHARM INC

  公开号：WO2007079239A2

  公开（公告）日：2007-07-12

  [EN] Disclosed herein are compounds of Formula I as defined herein, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, that modulates the activity of a ghrelin receptor. Disclosed herein are also methods of treating diseases or conditions that comprise administering to a subject in need thereof a therapeutically effective amount of a compound of Formula I.
  [FR] La présente invention concerne des composés de formule (I) tel que définie dans la description, ou un sel, ester, amide, ou prodrogue pharmaceutiquement acceptable de ceux-ci, qui assurent la modulation de l'activité d'un récepteur de ghréline. L'invention concerne également des procédés de traitement de maladies ou de pathologies comprenant l'administration à un sujet qui en a besoin d'une quantité thérapeutique d'un composé de formule (I).
• Indolylalkyltriphenylphosphonium Analogues Are Membrane-Depolarizing Mycobactericidal Agents
  作者：Ming Li、Samuel A. Nyantakyi、Pooja Gopal、Dinah binte Aziz、Thomas Dick、Mei-Lin Go

  DOI：10.1021/acsmedchemlett.7b00287

  日期：2017.11.9

  Agents that selectively target the mycobacterial membrane could potentially shorten treatment time for tuberculosis, reduce relapse, and curtail emergence of resistant strains. The lipophilicity and extensive charge-delocalized state of the triphenylphosphonium cation strongly favor accumulation within bacterial membranes. Here, we explored the antimycobacterial activities and membrane-targeting properties of indolylalkyltriphenylphosphonium analogues. The most active analogues preferentially inhibited growth of Mycobacterium tuberculosis H37Rv (MIC50 2-4 mu M) and were bactericidal against Mycobacterium bovis BCG (MBC99 3 mu M). In spite of their propensity to accumulate within membranes, we found no evidence that these compounds permeabilized mycobacterial membranes or induced cell-envelope stress. Our investigations indicated that their bacterical effects stem from sustained depolarization of mycobacterial membranes and ensuing disruptive effects on electron transfer and cell division.
• WO2007/79239
  申请人：——

  公开号：——

  公开（公告）日：——