4-tert-butyl-N-(4-piperazin-1-yl-quinolin-6-yl)benzenesulfonamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 4-tert-butyl-N-(4-piperazin-1-yl-quinolin-6-yl)benzenesulfonamide
• 英文别名: 4-tert-butyl-N-(4-piperazin-1-ylquinolin-6-yl)benzenesulfonamide
• 化学式: C₂₃H₂₈N₄O₂S
• 分子量: 424.567
• InChiKey: SHILVAMBAMVDBR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  82.7
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  4-氯-6-硝基喹啉 在 palladium on activated charcoal 吡啶 、 盐酸 、 氢气 、 potassium carbonate 作用下， 以 四氢呋喃 、 乙醇 、 二氯甲烷 、 甲苯 为溶剂， 反应 145.5h， 生成 4-tert-butyl-N-(4-piperazin-1-yl-quinolin-6-yl)benzenesulfonamide
  参考文献：
  名称：

  Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT6 receptor

  摘要：

  The discovery of (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides and their binding affinites for a selection of 5-HT and dopamine subreceptors is described. Many compounds show high afffinity (pK(i) > 8) for the 5-HT6 receptor and > 100-fold selectivity against a range of other receptors. Structure-activity relationships of these compounds are discussed. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(01)00558-3

文献信息

• Use
  申请人：——

  公开号：US20030166663A1

  公开（公告）日：2003-09-04

  The invention provides methods of treatment or prophylaxis of obesity, or methods of treatment for the reduction of food intake, comprising administering to a patient in need of such treatment a therapeutically effective amount of a sulfonamide compound of Formula I: 1 wherein the substituents are as described in the specification.

  本发明提供了治疗或预防肥胖症的方法，或减少食物摄入量的治疗方法，包括向需要这种治疗的患者施用治疗有效量的式 I 的磺酰胺化合物： 1 其中取代基如说明书所述。
• SULFONAMIDE DERIVATIVES
  申请人：SMITHKLINE BEECHAM PLC

  公开号：EP1228066A2

  公开（公告）日：2002-08-07
• USE OF SULFONAMIDE DERIVATIVES IN THE TREATMENT OF OBESITY OR FOR THE REDUCTION OF FOOD INTAKE
  申请人：BIOVITRUM AB

  公开号：EP1450806A1

  公开（公告）日：2004-09-01
• [EN] NOVEL COMPOUNDS<br/>[FR] NOUVEAUX COMPOSES
  申请人：SMITHKLINE BEECHAM PLC

  公开号：WO2001032646A2

  公开（公告）日：2001-05-10

  Novel sulfonamide compounds having CNS activity, processes for their preparation, to compositions containing the same and their use as medicaments.
• [EN] USE OF SULFONAMIDE DERIVATIVES IN THE TREATMENT OF OBESITY OR FOR THE REDUCTION OF FOOD INTAKE<br/>[FR] UTILISATION DE DERIVES SULFONAMIDE DANS LE TRAITEMENT DE L'OBESITE OU POUR LA REDUCTION DE PRISE D'ALIMENTS
  申请人：BIOVITRUM AB

  公开号：WO2003039547A1

  公开（公告）日：2003-05-15

  The invention provides a method of treatment or prophylaxis of obesity or for the reduction of food intake, comprising administering to a patient in need of such treatment a therapeutically effective amount of a sulfonamide compound of formula (I). Wherein the substituents are described in the specification.