1-(4-chlorobenzenesulfonyl)-3-methylpiperidine

• 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: 1-(4-chlorobenzenesulfonyl)-3-methylpiperidine
• 英文别名: 1-(4-chloro-benzenesulfonyl)-3-methyl-piperidine；1-[(4-Chlorophenyl)sulfonyl]-3-methylpiperidine；1-(4-chlorophenyl)sulfonyl-3-methylpiperidine
• 化学式: C₁₂H₁₆ClNO₂S
• 分子量: 273.784
• InChiKey: BNGKTBVBWYCKAF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  4-氯苯磺酰氯 、 3-甲基哌啶 在 吡啶 作用下， 反应 2.0h， 以43.5%的产率得到1-(4-chlorobenzenesulfonyl)-3-methylpiperidine
  参考文献：
  名称：

  In Vitro and in Vivo Antileishmanial and Trypanocidal Studies of New N-Benzene- and N-Naphthalenesulfonamide Derivatives

  摘要：

  We report in vivo and in vitro antileishmanial and trypanocidal activities of a new series of N-substituted benzene and naphthalenesulfonamides 1-15. Compounds 1-15 were screened in vitro against Leishmania infantum, Leishmania braziliensis, Leishmania guyanensis, Leishmania amazonensis, and Trypanosoma cruzi. Sulfonamides 6e, 10b, and 10d displayed remarkable activity and selectivity toward T. cruzi epimastigotes and amastigotes. 6e showed significant trypanocidal activity on parasitemia in a murine model of acute Chagas disease. Moreover, 6e, 8c, 9c, 12c, and 14d displayed interesting IC50 values against Leishmania spp promastigotes as well as L. amazonensis and L. infantum amastigotes. 9c showed excellent in vivo activity (up to 97% inhibition of the parasite growth) in a short-term treatment murine model for acute infection by L. infantum. In addition, the effect of compounds 9c and 14d on tubulin as potential target was assessed by confocal microscopy analysis applied to L. infantum promastigotes.

  DOI：

  10.1021/jm4006127

文献信息

• Heterocyclic Compounds Which Modulate The CB2 Receptor
  申请人：Bartolozzi Alessandra

  公开号：US20110312944A1

  公开（公告）日：2011-12-22

  Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

  本发明揭示了调节CB2受体的化合物。根据本发明，这些化合物与CB2受体结合并作为激动剂，用于治疗炎症。那些作为激动剂的化合物还可用于治疗疼痛。
• N-cyclic sulfonamido inhibitors of gamma secretase
  申请人：Neitzel L. Martin

  公开号：US20060035884A1

  公开（公告）日：2006-02-16

  The invention provides N-cyclic sulfonamido compounds for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula I, wherein R 4 , R 5 , R 6 , R 7 , and R 8 , are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula I.

  本发明提供了用于治疗或预防认知障碍（如阿尔茨海默病）的 N-环磺酰胺基化合物。 特别感兴趣的化合物由式 I 定义，其中 R 4 , R 5 , R 6 , R 7 和 R 8 如说明书所述。本发明还包括由式 I 化合物组成的药物组合物，以及使用式 I 化合物治疗认知障碍（包括阿尔茨海默病）的方法。
• N-CYCLIC SULFONAMIDO INHIBITORS OF GAMMA SECRETASE
  申请人：ELAN PHARMACEUTICALS, INC.

  公开号：EP1758884A2

  公开（公告）日：2007-03-07
• US8889670B2
  申请人：——

  公开号：US8889670B2

  公开（公告）日：2014-11-18
• [EN] N-CYCLIC SULFONAMIDO INHIBITORS OF GAMMA SECRETASE<br/>[FR] INHIBITEURS SULFONAMIDO N-CYCLIQUES DE GAMMA-SECRETASE
  申请人：ELAN PHARM INC

  公开号：WO2005113542A2

  公开（公告）日：2005-12-01

  The invention provides N-cyclic sulfonamido compounds for use in treating or preventing cognitive disorders, such as Alzheimer’s Disease. Compounds of particular interest are defined by Formula (I), wherein R4, R5, R6, R7 and R8 are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer’s disease using compounds of Formula (I).