Nα,Nε-di-(4-bromobenzenesulfonyl)-L-lysine | 359780-12-4

• 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: Nα,Nε-di-(4-bromobenzenesulfonyl)-L-lysine
• 英文别名: Nalpha,Nepsilon-di-(4-bromobenzenesulfonyl)-L-lysine；(2S)-2,6-bis[(4-bromophenyl)sulfonylamino]hexanoic acid
• CAS: 359780-12-4
• 化学式: C₁₈H₂₀Br₂N₂O₆S₂
• 分子量: 584.307
• InChiKey: MNFIXKOUKUIAKO-KRWDZBQOSA-N

物化性质

• 沸点：
  714.5±70.0 °C(Predicted)
• 密度：
  1.694±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  30
• 可旋转键数：
  11
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  146
• 氢给体数：
  3
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  Nα,Nε-di-(4-bromobenzenesulfonyl)-L-lysine 、 4-氟溴苄 以to yield 85% of the desired product的产率得到Nα,Nε-di-(4-bromobenzenesulfonyl)-Nε-(4-fluorobenzyl)-L-lysine
  参考文献：
  名称：

  Amino acid derivatives useful for the treatment of alzheimer's disease

  摘要：

  本发明涉及一种治疗阿尔茨海默病和其他疾病，和/或抑制β-分泌酶酶，和/或抑制哺乳动物体内Aβ肽沉积的方法，使用已知的式(I)化合物，其中R1、R2、R3、R4、W和Cx在此定义。

  公开号：

  US20060079550A1
• 作为产物：
  描述：

  L-赖氨酸 、 4-溴苯磺酰氯 在 sodium hydroxide 作用下， 以 水 为溶剂， 生成 Nα,Nε-di-(4-bromobenzenesulfonyl)-L-lysine
  参考文献：
  名称：

  Novel bis-(arylsulfonamide) hydroxamate-based selective MMP inhibitors

  摘要：

  A series of bis-(arylsulfonamide) hydroxamate inhibitors were synthesized. These compounds exhibit good potency against MMP-7 and MMP-9 depending on the nature, steric bulk, and substitution pattern of the substituents in the benzene ring. In general, the preliminary structure-activity relationships (SAR) suggest that among the DAPA hydroxamates (i) electron-rich benzene rings of the sulfonamides may produce better inhibitors than electron-poor analogs. However, potential H-bond acceptors can reverse the trend depending on the isozyme; (ii) isozyme selectivity between MMP-7 and-9 can be conferred through steric bulk and substitution pattern of the substituents in the benzene ring, and (iii) the MMP-10 inhibition pattern of the compounds paralleled that for MMP-9. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.04.035

文献信息

• Amino acid derivatives as HIV aspartyl protease inhibitors
  申请人：Pharmacor Inc.

  公开号：US06455587B1

  公开（公告）日：2002-09-24

  The present invention relates to a class of amino acid derivatives with HIV aspartyl protease inhibitory properties.

  本发明涉及一类具有HIV天冬氨酸蛋白酶抑制性能的氨基酸衍生物。
• Novel bis-(arylsulfonamide) hydroxamate-based selective MMP inhibitors
  作者：Rajesh Subramaniam、Manas K. Haldar、Shakila Tobwala、Bratati Ganguly、D.K. Srivastava、Sanku Mallik

  DOI：10.1016/j.bmcl.2008.04.035

  日期：2008.6

  A series of bis-(arylsulfonamide) hydroxamate inhibitors were synthesized. These compounds exhibit good potency against MMP-7 and MMP-9 depending on the nature, steric bulk, and substitution pattern of the substituents in the benzene ring. In general, the preliminary structure-activity relationships (SAR) suggest that among the DAPA hydroxamates (i) electron-rich benzene rings of the sulfonamides may produce better inhibitors than electron-poor analogs. However, potential H-bond acceptors can reverse the trend depending on the isozyme; (ii) isozyme selectivity between MMP-7 and-9 can be conferred through steric bulk and substitution pattern of the substituents in the benzene ring, and (iii) the MMP-10 inhibition pattern of the compounds paralleled that for MMP-9. (C) 2008 Elsevier Ltd. All rights reserved.
• Amino acid derivatives useful for the treatment of alzheimer's disease
  申请人：John Varghese

  公开号：US20060079550A1

  公开（公告）日：2006-04-13

  The present invention is a method of treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of known compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , W and C x are herein defined.

  本发明涉及一种治疗阿尔茨海默病和其他疾病，和/或抑制β-分泌酶酶，和/或抑制哺乳动物体内Aβ肽沉积的方法，使用已知的式(I)化合物，其中R1、R2、R3、R4、W和Cx在此定义。