1-Hydroxy-4-naphthalinsulfonsaeure-amid | 17284-44-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 1-Hydroxy-4-naphthalinsulfonsaeure-amid
• 英文别名: 4-hydroxy-naphthalene-1-sulfonic acid amide；4-Hydroxy-naphthalin-1-sulfonsaeure-amid；Naphthol-(1)-sulfonsaeure-(4)-amid；4-Hydroxy-1-naphthalenesulfonamide；4-hydroxynaphthalene-1-sulfonamide
• CAS: 17284-44-5
• 化学式: C₁₀H₉NO₃S
• mdl: MFCD00459105
• 分子量: 223.252
• InChiKey: WOIJKOZDDUWHBG-UHFFFAOYSA-N

物化性质

• 熔点：
  217 °C(Solv: ethanol (64-17-5))
• 沸点：
  494.6±47.0 °C(Predicted)
• 密度：
  1.479±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  88.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-Hydroxy-4-naphthalinsulfonsaeure-amid 、 环氧氯丙烷 以11%的产率得到
  参考文献：
  名称：

  RAULS D. O.; BAKER J. K., J. MED. CHEM., 1979, 22, NO 1, 81-86

  摘要：

  DOI：
• 作为产物：
  描述：

  4-ethoxycarbonyloxy-naphthalene-1-sulfonyl chloride 生成 1-Hydroxy-4-naphthalinsulfonsaeure-amid
  参考文献：
  名称：

  Relationship of nonspecific antiarrhythmic and negative inotropic activity with physicochemical parameters of propranolol analogs

  摘要：

  In an attempt to separate the nonspecific antiarrhythmic activity of propranolol from its negative inotropic effects, analogues containing hydrophilic and lipophilic substituents on the nitrogen and on the naphthyl ring were prepared and tested in an isolated tissue preparation. Though it had been predicted that analogues containing a very hydrophilic group on the nitrogen would have the highest antiarrhythmic/negative inotropic effect ratio, it was found that both effects increased identically when the lipophilicity of either the nitrogen or ring substituent was increased.

  DOI：

  10.1021/jm00187a018

文献信息

• [EN] NOVEL N-ACYL-ARYLSULFONAMIDE DERIVATIVES AS AMINOACYL-TRNA SYNTHETASE INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS DE N-ACYL-ARYLSULFONAMIDE UTILISÉS EN TANT QU'INHIBITEURS D'AMINOACYL-ARNT SYNTHÉTASE
  申请人：LATVIAN INST ORGANIC SYNTHESIS

  公开号：WO2016129983A1

  公开（公告）日：2016-08-18

  The present invention relates to novel N-acyl-diarysulfonamides acting as inhibitors of bacterial aminoacyl-tRNA synthetase. These can be used as medicines or as constituent of medicines for the treatment of bacterial infections.

  本发明涉及作为细菌氨酰-tRNA合成酶抑制剂的新型N-酰基二芳基磺酰胺。这些可以用作药物或药物成分，用于治疗细菌感染。
• [EN] SUBSTITUTED ACYL SULFONAMIDES FOR TREATING CANCER<br/>[FR] ACYLSULFONAMIDES SUBSTITUÉS POUR LE TRAITEMENT DU CANCER
  申请人：BROAD INST INC

  公开号：WO2022081807A1

  公开（公告）日：2022-04-21

  The present invention provides acyl sulfonamide compounds of general formula (I): in which R1, R2, R3, R4, R5, R6· Raand Rbare as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treatment and/or prophylaxis of diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.

  本发明提供了通式（I）的酰基磺酰胺化合物：其中，R1、R2、R3、R4、R5、R6·Ra和Rb如本文所述和定义，以及制备该化合物的方法，用于制备该化合物的中间体化合物，包含该化合物的药物组合物和组合物，以及使用该化合物制造用于治疗或预防疾病的药物组合物，特别是治疗过度增生性疾病的药物组合物，作为唯一的活性成分或与其他活性成分组合使用，以及治疗和/或预防疾病的方法，特别是癌症，更特别是KAT6A和/或KAT6B局部扩增的癌症，其中该方法包括向需要该方法的受体中施用至少一种通式（I）的有效量化合物。
• Compositions for repelling crawling insects
  申请人：——

  公开号：US20020094993A1

  公开（公告）日：2002-07-18

  The present invention relates to novel compositions, comprising a repellent and an additive, where the additive is selected from the group consisting of phenol, benzaldehyde, benzoic acid or derivatives thereof and is present in a ratio of from 10:100 to 200:100% by weight to the repellent, and to their use for repelling crawling harmful insects, in particular ants or cockroaches.

  本发明涉及新型组合物，包括一种驱虫剂和一种添加剂，其中所述添加剂选自苯酚、苯甲醛、苯甲酸或其衍生物组成的群体，并以10:100至200:100％重量的比例存在于驱虫剂中，以及其用于驱赶爬行有害昆虫，特别是蚂蚁或蟑螂。
• N-acyl-arylsulfonamide derivatives as aminoacyl-tRNA synthetase inhibitors
  申请人：Oxford Drug Design Limited

  公开号：US11072581B2

  公开（公告）日：2021-07-27

  The present invention relates to novel N-acyl-diarysulfonamides acting as inhibitors of bacterial aminoacyl-tRNA synthetase. These can be used as medicines or as constituent of medicines for the treatment of bacterial infections.

  本发明涉及作为细菌氨基酰-tRNA 合成酶抑制剂的新型 N-酰基二亚磺酰胺类化合物。这些药物可用作治疗细菌感染的药物或药物成分。
• Hiyama, Yakugaku Zasshi/Journal of the Pharmaceutical Society of Japan, 1952, vol. 72, p. 1370,1373
  作者：Hiyama

  DOI：——

  日期：——