N-(4-chloro-3-sulfamoylphenyl)formamide | 1370347-18-4

• 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: N-(4-chloro-3-sulfamoylphenyl)formamide
• CAS: 1370347-18-4
• 化学式: C₇H₇ClN₂O₃S
• 分子量: 234.663
• InChiKey: JKKOILRABSNGMF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  97.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N-(4-chloro-3-sulfamoylphenyl)formamide 、 phenyl (4-methylpyrimidin-2-yl)carbamate 在 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 乙腈 为溶剂， 以46%的产率得到N-(4-chloro-3-(N-(4-methylpyrimidin-2-ylcarbamoyl)sulfamoyl)phenyl)formamide
  参考文献：
  名称：

  Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents

  摘要：

  A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by H-1 NMR, C-13 NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC50 against THP-1 cells greater than 100 mg/L. (C) 2012 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2012.01.011
• 作为产物：
  描述：

  2-chloro-5-nitrobenzenesulphonic acid sodium salt 在 氯磺酸 、 甲酸 、 palladium 10% on activated carbon 、 氨 、 氢气 作用下， 以 四氢呋喃 、 甲醇 、 水 为溶剂， 反应 18.0h， 生成 N-(4-chloro-3-sulfamoylphenyl)formamide
  参考文献：
  名称：

  Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents

  摘要：

  A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by H-1 NMR, C-13 NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC50 against THP-1 cells greater than 100 mg/L. (C) 2012 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2012.01.011

文献信息

• Compounds
  申请人：Liebeschuetz Walter John

  公开号：US20050032790A1

  公开（公告）日：2005-02-10

  Compounds of formula (I) where R 2 , each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.

  式(I)的化合物中，其中R2、每个X、L、Y、Cy、Lp、D和n的定义如规范中所述，是丝氨酸蛋白酶抑制剂，可用作抗血栓剂。
• SERINE PROTEASE INHIBITORS
  申请人：ELI LILLY AND COMPANY

  公开号：EP1192132A2

  公开（公告）日：2002-04-03
• US6855715B1
  申请人：——

  公开号：US6855715B1

  公开（公告）日：2005-02-15
• [EN] COMPOUNDS<br/>[FR] COMPOSES
  申请人：LILLY CO ELI

  公开号：WO2000076970A2

  公开（公告）日：2000-12-21

  Use of compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, as serine protease inhibitors.
• Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents
  作者：Li Pan、Ying Jiang、Zhen Liu、Xing-Hai Liu、Zhuo Liu、Gang Wang、Zheng-Ming Li、Di Wang

  DOI：10.1016/j.ejmech.2012.01.011

  日期：2012.4

  A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by H-1 NMR, C-13 NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC50 against THP-1 cells greater than 100 mg/L. (C) 2012 Elsevier Masson SAS. All rights reserved.