N1-tosyl-spermine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N1-tosyl-spermine
• 英文别名: N-[3-[4-(3-aminopropylamino)butylamino]propyl]-4-methylbenzenesulfonamide
• 化学式: C₁₇H₃₂N₄O₂S
• 分子量: 356.533
• InChiKey: VNFBDCKDOHSIQR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  24
• 可旋转键数：
  14
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  105
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  精胺 、 对甲苯磺酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 生成 N1-tosyl-spermine
  参考文献：
  名称：

  Structural correlation between lipophilicity and lipopolysaccharide-sequestering activity in spermine-sulfonamide analogs

  摘要：

  Lipopolysaccharides (LPS), otherwise termed 'endotoxins', are outer-membrane constituents of Gram-negative bacteria, and play a key role in the pathogenesis of 'Septic Shock', a major cause of mortality in the critically ill patient. We had previously defined the pharmacophore necessary for small molecules to specifically bind and neutralize this complex carbohydrate. A series of aryl and aliphatic spermine-sulfonamide analogs were synthesized and tested in a series of binding and cell-based assays in order to probe the effect of lipophilicity on sequestration ability. A strong correlation was indeed found, supporting the hypothesis that endotoxin-neutralizing ability involves a lipophilic or membrane attachment event. The research discussed herein may be useful for the design of additional carbohydrate recognizing molecules and endotoxin-neutralizing drugs. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2006.09.026

文献信息

• Methods and compositions for treatment of demyelinating diseases
  申请人：Pathologica LLC

  公开号：US10350178B2

  公开（公告）日：2019-07-16

  Disclosed herein is a method of prevention of progression of a multiple sclerosis in a patient, comprising the administration of methylglyoxal bis(guanylhydrazone) (MGBG) to the patient in need thereof. Also disclosed herein is a method of prevention or reduction in severity of the initiation phase of autoimmune response in a patient having multiple sclerosis, comprising the administration of MGBG to the patient in need thereof.

  本文公开了一种预防多发性硬化症患者病情恶化的方法，包括向有需要的患者施用甲基乙二醛双（鸟苷酸腙）（MGBG）。本文还公开了一种预防多发性硬化症患者自身免疫反应起始阶段或减轻其严重程度的方法，包括对有需要的患者施用 MGBG。
• NOVEL POLYAMINE DERIVATIVES
  申请人：Miyake Muneharu

  公开号：US20100063322A1

  公开（公告）日：2010-03-11

  A compound having the general formula (I) or a pharmacologically acceptable salt thereof: X—NH—Y—NH—R 1 (I) [wherein X represents R 2 —SO 2 — in which R 2 represents an optionally substituted lower alkyl group or phenyl group; Y represents a group selected from the group consisting of —R 3 —NH—R 4 —, —R 5 —NH—R 6 —NH—R 7 —, —R 8 —NH—R 9 —NH—R 10 —NH—R 11 — and —R 12 —NH—R 13 —NH—R 14 —NH—R 15 — in which R 3 to R 15 each independently represent a C 3 to C 5 alkylene group; and R 1 represents hydrogen or an optionally substituted lower alkyl group, with the proviso that the case where X represents a tosyl group, Y represents —(CH 2 ) 3 —NH—(CH 2 ) 4 —NH—(CH 2 ) 3 — and R 1 represents hydrogen is excepted].
• PHARMACEUTICAL FOR ORAL DELIVERY COMPRISING MGBG AND METHODS OF TREATING DISEASE
  申请人：McKearn John

  公开号：US20110112199A1

  公开（公告）日：2011-05-12

  Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.
• METHODS AND COMPOSITIONS FOR TREATMENT OF DEMYELINATING DISEASES
  申请人：PATHOLOGICA LLC

  公开号：US20150359761A1

  公开（公告）日：2015-12-17

  Disclosed herein are new oral pharmaceutical compositions of SAMDC inhibitors, polyamine analogs, and polyamine biosynthesis inhibitors, and their application for the treatment of conditions including demyelinating diseases, autoimmune disorders affecting the nervous system, and other neurodegenerative conditions.
• US5342945A
  申请人：——

  公开号：US5342945A

  公开（公告）日：1994-08-30