3-acetylamino-benzenesulfonic acid amide | 23010-42-6

• 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: 3-acetylamino-benzenesulfonic acid amide
• 英文别名: 3-Acetylamino-benzolsulfonsaeure-amid；(N-Acetyl-anilin-sulfonsaeure-(3))-amid；3-Acetamino-benzol-sulfonsaeure-(1)-amid；N-[3-(aminosulfonyl)phenyl]-acetamide；N-(3-sulfamoylphenyl)acetamide
• CAS: 23010-42-6
• 化学式: C₈H₁₀N₂O₃S
• mdl: MFCD03987222
• 分子量: 214.245
• InChiKey: ZMXZWFNWSWLMFN-UHFFFAOYSA-N

物化性质

• 熔点：
  216-219 °C(Solv: acetic acid (64-19-7))
• 密度：
  1.414±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.125
• 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：

  3-acetylamino-benzenesulfonic acid amide 、 异氰酸正丁酯 在 三乙胺 作用下， 生成 1-(3-Acetamino-benzolsulfonyl)-3-butyl-harnstoff
  参考文献：
  名称：

  Hoekfelt,B.; Joensson,A., Journal of medicinal and pharmaceutical chemistry, 1962, vol. 5, p. 231 - 239

  摘要：

  DOI：
• 作为产物：
  描述：

  3-乙酰基氨基苯磺酰氯 在 氨 作用下， 生成 3-acetylamino-benzenesulfonic acid amide
  参考文献：
  名称：

  Jacobs; Heidelberger, Journal of the American Chemical Society, 1917, vol. 39, p. 2437

  摘要：

  DOI：

文献信息

• Useful Combinations of Monobactam Antibiotics With Beta-Lactamase Inhibitors
  申请人：Desarbre Eric

  公开号：US20100056478A1

  公开（公告）日：2010-03-04

  A pharmaceutically composition, comprising a combination of an antibiotically active compound of the formula (I): with a β-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another β-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).

  一种药物组合物，包括公式（I）的抗生素活性化合物与公式（II）至（XIII）中的β-内酰胺酶抑制剂的组合，对革兰氏阴性菌具有活性，特别是对已经对阿奇霉素、卡鲁莫南和替吉奴等抗生素产生耐药性的细菌具有活性。该组合物还可以包含公式（II）至（XIII）中的另一种β-内酰胺酶抑制剂，特别是公式（V）或公式（VI）的β-内酰胺酶抑制剂。
• COMPOUNDS THAT INHIBIT HIF-1 ACTIVITY, THE METHOD FOR PREPARATION THEREOF AND THE PHARMACEUTICAL COMPOSITION CONTAINING THEM AS AN EFFECTIVE COMPONENT
  申请人：Lee Jung Joon

  公开号：US20090306078A1

  公开（公告）日：2009-12-10

  Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.

  本文披露了一种HIF-1抑制剂，其制备方法以及包含其作为活性成分的药物组合物。该HIF-1抑制剂通过对HIF-1的抑制活性显示出抗癌活性，HIF-1是一种转录因子，在癌症的生长和转移中起重要作用，但不具有一般细胞毒性。因此，该HIF抑制剂及其药学上可接受的盐可用作各种癌症（如肝癌、胃癌和乳腺癌）的治疗剂。此外，具有HIF-1抑制活性的化合物对于治疗由HIF-1介导的VEGF表达加重的糖尿病视网膜病变和关节炎非常有用。
• Compounds that inhibit HIF-1 activity, the method for preparation thereof and the pharmaceutical composition containing them as an effective component
  申请人：Lee Jung Joon

  公开号：US08394799B2

  公开（公告）日：2013-03-12

  Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.

  本发明涉及一种HIF-1抑制剂，其制备方法以及包含该抑制剂作为活性成分的制药组合物。该HIF-1抑制剂通过对HIF-1的抑制活性表现出抗癌活性，HIF-1是一种转录因子，在癌症的生长和转移中起着重要作用，但不具有普遍的细胞毒性。因此，HIF抑制剂及其药学上可接受的盐可以用作各种癌症（如肝癌、胃癌和乳腺癌）的治疗剂。此外，具有对HIF-1抑制活性的化合物对于治疗由HIF-1介导的VEGF表达加重的糖尿病视网膜病变和关节炎非常有用。
• USEFUL COMBINATIONS OF MONOBACTAM ANTIBIOTICS WITH BETA-LACTAMASE INHIBITORS
  申请人：Basilea Pharmaceutica AG

  公开号：US20150031662A1

  公开（公告）日：2015-01-29

  A pharmaceutical composition, comprising a combination of an antibiotically active compound of the formula (I): with a β-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another β-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).

  一种药物组合物，包括式(I)的抗生素活性化合物与式(II)至式(XIII)中的一种β-内酰胺酶抑制剂的组合，对革兰氏阴性菌有活性，特别是对已经对阿奇霉素、卡鲁莫纳和替莫纳等抗生素产生耐药性的细菌有活性。该组合物可以包括另一种式(II)至式(XIII)中的β-内酰胺酶抑制剂，特别是式(V)或式(VI)的β-内酰胺酶抑制剂。
• Ferric Chloride-Mediated Transacylation of <i>N</i>-Acylsulfonamides
  作者：Dayong Sang、Bingqian Dong、Kangkang Yu、Juan Tian

  DOI：10.1021/acs.joc.3c02288

  日期：2024.2.16

  Transacylation of N-acylsulfonamides, which replaces the N-acyl group with a new one, is a challenging and underdeveloped fundamental transformation. Herein, a general method for transacylation of N-acylsulfonamides is presented. The transformation is enabled by coincident catalytic reactivities of FeCl3 for nonhydrolytic deacylation of N-acylsulfonamides and subsequent acylation of the resultant sulfonamides

  N-酰基磺酰胺的酰基转移，即用一个新的 N-酰基取代N-酰基，是一种具有挑战性且尚未发展的根本性转变。本文提出了N-酰基磺酰胺转酰基的一般方法。该转化是通过FeCl 3对N-酰基磺酰胺的非水解脱酰化和随后所得磺酰胺的酰化的同时催化反应性实现的，并且可以逐步或以一锅方式进行。 GaCl 3和RuCl 3 · xH 2 O对该反应同样有效。该方法温和、高效、操作简单。各种官能团（例如卤素、酮、硝基、氰基、醚和酯）具有良好的耐受性，从而提供良好至优异的收率的转酰化产物。