(4-nitro-benzoyl)-sulfanilyl-amine | 748816-33-3

• 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: (4-nitro-benzoyl)-sulfanilyl-amine
• 英文别名: 4-Nitro-benzoesaeure-sulfanilylamid；(4-Nitro-benzoyl)-sulfanilyl-amin；4-Nitro-N-sulfanilyl-benzamid；p-Nitro-N-sulfanilylbenzamide；N-(4-aminophenyl)sulfonyl-4-nitrobenzamide
• CAS: 748816-33-3
• 化学式: C₁₃H₁₁N₃O₅S
• 分子量: 321.313
• InChiKey: HLIRSRUFQBURJT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  144
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (4-nitro-benzoyl)-sulfanilyl-amine 、 乙酸酐 生成 N-acetyl-sulfanilic acid-(4-nitro-benzoylamide)
  参考文献：
  名称：

  Proteolytic processing of human growth hormone (GH) by rat tissues in vitro: Influence of sex and age

  摘要：

  Although a wealth of evidence exists indicating that proteolytic cleavage can enhance the biological activity of the growth hormone (GH) molecule, the mechanisms responsible for the generation of GH fragments are not completely understood. In the present work we investigated the ability of different rat tissues to cleave 22 kDa GH, as well as the influence of sex and age, the two major physiological regulators of GH secretion on this process. Our results show that tissue homogenates obtained from rat liver, skeletal muscle or adipose tissue (three well-documented target organs for the hormone) are able to cleave 22K-GH, while the hormone is resistant to cleavage by rat brain homogenates. This process is rather selective for 22K-GH, since the 20 kDa GH variant exhibits stability to degradation by all tissue homogenates investigated. Moreover, only a minor fraction of 22 kDa GH is cleaved under our experimental conditions, suggesting that GH microheterogeneity within the 22 kDa range may also determine hormone susceptibility. Finally, we also found that 22K-GH processing shows important age-related changes (the greatest intensity observed in 4-day-old pups), while no gender-related differences exist in any of the tissues investigated. (C) 2000, Editrice Kurtis.

  DOI：

  10.1007/bf03345065
• 作为产物：
  描述：

  N-(4-nitro-benzoyl)-sulfanilic acid-(4-nitro-benzoylamide) 在 sodium hydroxide 作用下， 生成 (4-nitro-benzoyl)-sulfanilyl-amine
  参考文献：
  名称：

  Chemotherapeutic Study of p-Nitrobenzoyl- and Related Compounds

  摘要：

  DOI：

  10.1021/ja01251a029

文献信息

• <i>N</i>-Acylsulfonamide: a valuable moiety to design new sulfa drug analogues
  作者：Romain Amador、Ali Tahrioui、Magalie Barreau、Olivier Lesouhaitier、Michael Smietana、Guillaume Clavé

  DOI：10.1039/d3md00229b

  日期：——

  Sulfonamides are the oldest class of antibiotics, discovered more than 80 years ago. They are still used today despite the appearance of drug resistance phenomena that limit their prescription. Since the discovery and use of the first sulfa drugs, many analogues have been synthesized in order to obtain new active molecules able to circumvent bacterial resistance. Structurally similar to sulfonamide

  磺胺类药物是最古老的一类抗生素，已于 80 多年前被发现。尽管耐药现象的出现限制了它们的处方，但它们至今仍在使用。自从第一个磺胺药物的发现和使用以来，已经合成了许多类似物，以获得能够规避细菌耐药性的新活性分子。 N-酰基磺酰胺基团与磺酰胺结构相似，由于其特定的物理化学性质而引起了药物化学领域的兴趣。我们在此报告了 18 种具有N-酰基磺酰胺部分的磺胺药物类似物的合成和抗菌/抗生物膜活性。这些衍生物是通过容易获得的硫代酸和磺酰叠氮合成子之间的磺基点击反应有效获得的。
• Sulfanilamide Derivatives. IV. N¹,N⁴-Diacylsulfanilamides and N¹-Acylsulfanilamides
  作者：M. L. Crossley、E. H. Northey、Martin E. Hultquist

  DOI：10.1021/ja01265a107

  日期：1939.10.1
• Chemotherapeutic Study of p-Nitrobenzoyl- and Related Compounds
  作者：C. Siebenmann、R. J. Schnitzer

  DOI：10.1021/ja01251a029

  日期：1943.11
• Proteolytic processing of human growth hormone (GH) by rat tissues in vitro: Influence of sex and age
  作者：M. García-Barros、J. Devesa、Víctor M. Arce

  DOI：10.1007/bf03345065

  日期：2000.12

  Although a wealth of evidence exists indicating that proteolytic cleavage can enhance the biological activity of the growth hormone (GH) molecule, the mechanisms responsible for the generation of GH fragments are not completely understood. In the present work we investigated the ability of different rat tissues to cleave 22 kDa GH, as well as the influence of sex and age, the two major physiological regulators of GH secretion on this process. Our results show that tissue homogenates obtained from rat liver, skeletal muscle or adipose tissue (three well-documented target organs for the hormone) are able to cleave 22K-GH, while the hormone is resistant to cleavage by rat brain homogenates. This process is rather selective for 22K-GH, since the 20 kDa GH variant exhibits stability to degradation by all tissue homogenates investigated. Moreover, only a minor fraction of 22 kDa GH is cleaved under our experimental conditions, suggesting that GH microheterogeneity within the 22 kDa range may also determine hormone susceptibility. Finally, we also found that 22K-GH processing shows important age-related changes (the greatest intensity observed in 4-day-old pups), while no gender-related differences exist in any of the tissues investigated. (C) 2000, Editrice Kurtis.