1-(2-chlorophenyl)sulfonylpiperazine | 233261-84-2

• 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-(2-chlorophenyl)sulfonylpiperazine
• 英文别名: 1-((2-Chlorophenyl)sulfonyl)piperazine
• CAS: 233261-84-2
• 化学式: C₁₀H₁₃ClN₂O₂S
• mdl: MFCD06351003
• 分子量: 260.744
• InChiKey: BVKKRWPRNWNKTH-UHFFFAOYSA-N

物化性质

• 熔点：
  63～66℃

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  57.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(2-chlorophenyl)sulfonylpiperazine 在 盐酸 、 potassium carbonate 作用下， 以 四氢呋喃 、 乙醚 、 二氯甲烷 为溶剂， 反应 72.0h， 生成 1-benzo[b]thiophen-3-yl-3-[4-(2-chlorobenzenesulfonyl)piperazin-1-yl]propane-1-one hydrochloride
  参考文献：
  名称：

  Novel Benzo[b]thiophene Derivatives as New Potential Antidepressants with Rapid Onset of Action

  摘要：

  We report benzo[b]thiophene derivatives synthesized according 10 a dual strategy. 8j, 9c, and 9e with affinity values toward 5-HT(7)R and 5-HTT were selected to probe their antidepressant activity in vivo using the forced swimming text (FST). The results slowed significant antidepressant activity after chronic treatment. 9c was effective in reducing the immobility time in FST even after acute treatment. These findings identify these compounds as a new class of antidepressants with a rapid onset of action.

  DOI：

  10.1021/jm2000773
• 作为产物：
  描述：

  2-氯苯磺酰氯 在 盐酸 、 溶剂黄146 、 三乙胺 作用下， 以 二氯甲烷 、 水 为溶剂， 反应 50.0h， 生成 1-(2-chlorophenyl)sulfonylpiperazine
  参考文献：
  名称：

  Novel Benzo[b]thiophene Derivatives as New Potential Antidepressants with Rapid Onset of Action

  摘要：

  We report benzo[b]thiophene derivatives synthesized according 10 a dual strategy. 8j, 9c, and 9e with affinity values toward 5-HT(7)R and 5-HTT were selected to probe their antidepressant activity in vivo using the forced swimming text (FST). The results slowed significant antidepressant activity after chronic treatment. 9c was effective in reducing the immobility time in FST even after acute treatment. These findings identify these compounds as a new class of antidepressants with a rapid onset of action.

  DOI：

  10.1021/jm2000773

文献信息

• CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREOF
  申请人：Millennium Pharmaceuticals, Inc.

  公开号：US20160031908A1

  公开（公告）日：2016-02-04

  Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.

  揭示了新颖的化合物以及治疗与异常白细胞召集和/或激活相关的疾病的方法。该方法包括向需要的受试者施用代表的化合物的有效量： 或其生理上可接受的盐。
• Chemokine receptor anagonists and methods of use therefor
  申请人：Millennium Pharmaceuticals, Inc.

  公开号：US20020169155A1

  公开（公告）日：2002-11-14

  Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: 1 or physiologically acceptable salt thereof.

  揭示了新颖的化合物以及一种治疗与异常白细胞召集和/或激活相关疾病的方法。该方法包括向需要的受试者施用化合物1或其生理上可接受的盐的有效量。
• CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREFOR
  申请人：——

  公开号：US20020119973A1

  公开（公告）日：2002-08-29

  Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: 1 and physiologically acceptable salts thereof. 2

  披露了新颖的化合物以及一种治疗与异常白细胞招募和/或激活相关疾病的方法。该方法包括向需要治疗的主体施用一种有效量的化合物，该化合物由以下结构表示： 1 以及它们的生理可接受的盐。 2
• Chemokine receptor antagonists and methods of use thereof
  申请人：Luly R. Jay

  公开号：US20050070549A1

  公开（公告）日：2005-03-31

  Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: formula (1) or physiologically acceptable salt thereof.

  揭示了新化合物和一种治疗与异常白细胞召集和/或激活相关疾病的方法。该方法包括向需要的受试者施用由以下公式（1）表示的化合物或其生理上可接受的盐的有效量。
• Synthesis and antibacterial activity of novel myricetin derivatives containing sulfonylpiperazine
  作者：Jun He、Xue-Mei Tang、Ting-Ting Liu、Feng Peng、Qing Zhou、Li-Wei Liu、Ming He、Wei Xue

  DOI：10.1007/s11696-020-01363-3

  日期：2021.3

  Myricetin derivatives containing sulfonylpiperazine were synthesized and their structures were confirmed by NMR and HRMS. The antibacterial activity results indicated that some compounds showed good antibacterial activity against Xanthomonas oryzaepv. oryzae (Xoo), Xanthomonas axonopodispv. citri (Xac) and Ralstonia solanacearum (Rs). Among them, compounds 4m and 4p revealed excellent antibacterial activities

  合成了含有磺酰基哌嗪的杨梅素衍生物，并通过NMR和HRMS证实其结构。抗菌活性结果表明，某些化合物对米生黄单胞菌具有良好的抗菌活性。米（Xoo），黄单胞菌（Xanthomonas axonopodispv）。柠檬（Xac）和青枯菌（Rsstonia solanacearum）（Rs）。其中，化合物4m和4p对Rs表现出优异的抗菌活性，其浓度为最大作用浓度的50％（EC 50）值分别为4和4μg/ mL，优于对照药物比美噻唑（13μg/ mL）和硫二唑铜（185μg/ mL）。如使用扫描电子显微镜（SEM）所观察到的，这些化合物通过引起细菌表面的折叠和变形而起作用，从而导致细菌结构不完整，从而达到抑菌的目的。合成的杨梅素衍生物有望指导新型抗菌剂的研究方向。