leucinohydroxamic acid | 5699-68-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: leucinohydroxamic acid
• 英文别名: 2-Amino-4-methyl-pentansaeure-hydroxyamid；leucine hydroxyamide；DL-leucine hydroxyamide；DL-Leucin-hydroxyamid；2-amino-N-hydroxy-4-methylpentanamide
• CAS: 5699-68-3
• 化学式: C₆H₁₄N₂O₂
• 分子量: 146.189
• InChiKey: UJJHPFLWSVFLBE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  10
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  75.4
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  leucinohydroxamic acid 生成 N-benzoyl-leucine benzoyloxyamide
  参考文献：
  名称：

  Effect of acute elevation of IGF-I on circulating GH, TSH, insulin, IGF-II and IGFBP-3 levels in non-endocrine short stature (NESS)

  摘要：

  It is not clear whether acute and slight elevation of serum IGF-I, which does not affect blood glucose levels, modulates circulating GH levels. To clarify this, small doses of recombinant human IGF-I (rhIGF-I, 5 microg/kg, i.v.) were administered as a bolus to 10 children with non-endocrine short stature (NESS) (5 males and 5 females, 11.2+/-0.7 yr old) after an overnight fast. Physiological saline was administered intravenously to sex- and age-matched NESS controls (5 males and 5 females, 10.9+/-0.7 yr old). The changes of serum GH, TSH, PRL, IGF-I, IGF-II, IGFBP-3, T4, T3 and plasma glucose levels after the administration were compared to those of the control subjects. Serum IGF-I levels increased significantly from 15 to 150 min after injection compared to those in the control group. The peak value was observed at 15 min (delta increment, 74.6+/-11.8 microg/l). At 15 min after the injection, serum insulin was suppressed significantly (p<0.05), although plasma glucose levels were not modified significantly. Serum TSH showed a significant decrease by rhIGF-I at 15 min and 60 min, whereas serum T4 and T3 levels were not modified. Serum GH was also significantly suppressed at 60 min (p<0.02) and showed a rebound increase at 120 min (p<0.05). Serum IGFBP-3 levels after rhIGF-I were higher than controls at 90 min and 150 min. No significant changes of serum PRL, IGF-II, (IGF-I plus IGF-II)/IGFBP-3 ratios were observed after the IGF-I injection compared to controls. These results indicate that circulating IGF-I is a physiological regulator of GH secretion in normal children, since the changes of IGF-I after the small doses of rhlGF-I administration were within physiological ranges and did not affect plasma glucose levels.

  DOI：

  10.1007/bf03343801
• 作为产物：
  描述：

  乙基L-亮氨酸酯 在 羟胺 作用下， 生成 leucinohydroxamic acid
  参考文献：
  名称：

  环状异羟肟酸衍生物的合成及其螯合能力和生物活性。

  摘要：

  合成了几种环羟肟酸。它们表现出金属螯合能力和镇痛活性，符合预期。除了这些活性外，其中一些化合物还抑制了微生物的生长。

  DOI：

  10.1248/cpb.36.2323

文献信息

• Anticancer Activity of Spirocyclic Hydroxamic Acids (Derivatives of 1-Hydroxy-1,4,8-Triazaspiro[4,5]Decan-2-One), Histone Deacetylase Inhibitors
  作者：N. P. Akentieva、A. R. Gizatullin、S. A. Goncharova、T. A. Raevskaya、N. S. Goryachev、N. I. Shkondina、T. R. Prichodchenko、I. V. Vystorop、S. S. Shushanov

  DOI：10.1134/s1990747818040037

  日期：2019.1

  The effect of 10 racemic spirocyclic hydroxamic acids (CHA 1–10, derivatives of 1-hydroxy-1,4,8-triazaspiro[4,5]decan-2-one), containing pharmacophore imidazolidinone and piperidine fragments with different substituents, on the activity of enzyme histone deacetylase (HDAC) was studied. It was shown that CHA (1–10) inhibit HDAC activity in cultured breast cancer cells. It was shown that CHA (1–10) as

  10 种外消旋螺环异羟肟酸（CHA 1-10，1-羟基-1,4,8-三氮杂螺[4,5]癸烷-2-one 的衍生物），含有药效团咪唑啉酮和具有不同取代基的哌啶片段，对研究了酶组蛋白脱乙酰酶（HDAC）的活性。结果表明，CHA (1-10) 抑制培养的乳腺癌细胞中的 HDAC 活性。结果表明，CHA（1-10）作为顺铂和环磷烷多化学疗法的一部分在体内具有显着的化学增敏抗肿瘤活性。在体内肿瘤模型上获得的结果表明，CHA 可以被认为是肿瘤综合化疗的潜在药物成分。
• Arylsulfonamido-substituted hydroxamic acid derivatives
  申请人：Breitenstein Werner

  公开号：US20080275127A1

  公开（公告）日：2008-11-06

  α-Amino hydroxamic acid derivative of the formula I, in which R is C 2 -C 7 -alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C 3 -C 5 -cycloalkyl or unsubstituted or substituted C 3 -C 6 -heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C 3 -C 7 -alkenyl or C 3 -C 7 -alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C 3 -C 5 -cycloalkyl or unsubstituted or substituted C 3 -C 6 -heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; and the other symbols are as defined in claim 1, are described. These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasion) and pulmonary disorders (e.g. emphysema, COPD).

  本文描述了公式I的α-氨基羟肟酸衍生物，其中R是C2-C7烷基，可以是单取代、双取代或三取代的卤素、硝基、低酰氧基、三氟甲氧基、氰基、C3-C5环烷基或未取代或取代的C3-C6杂环芳基，其中所述杂环芳基包括一个或两个从O、S和N组成的杂原子；或者是C3-C7烯基或C3-C7炔基，每种情况下都未取代或单取代、双取代或三取代的卤素、硝基、低酰氧基、三氟甲氧基、氰基、C3-C5环烷基或未取代或取代的C3-C6杂环芳基，其中所述杂环芳基包括一个或两个从O、S和N组成的杂原子；其他符号如权利要求1中所定义。这些化合物是MMP，特别是MMP2的抑制剂，并可用于治疗MMP依赖性疾病，特别是炎症病症、类风湿性关节炎、骨关节炎、肿瘤（肿瘤生长、转移、进展或侵袭）和肺部疾病（例如肺气肿、COPD）。
• Hydroxamic Acid Derivatives, Preparation and Therapeutic Uses Thereof
  申请人：Khan Amin

  公开号：US20120004309A1

  公开（公告）日：2012-01-05

  Disclosed are amino alkyl/aryl hydroxamic acid compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for degenerative diseases in mammal.

  本发明公开了氨基烷基/芳基羟肟酸化合物及含有该类化合物的制药组合物。所公开的组合物可作为哺乳动物退行性疾病的治疗剂。
• Advanced drug development and manufacturing
  申请人：ICAGEN, LLC

  公开号：US10877035B2

  公开（公告）日：2020-12-29

  X-ray fluorescence (XRF) spectrometry has been used for detecting binding events and measuring binding selectivities between chemicals and receptors. XRF may also be used for estimating the therapeutic index of a chemical. For estimating the binding selectivities of a chemical versus chemical analogs, for measuring post translational modification of proteins, and for drug manufacturing.

  X 射线荧光 (XRF) 光谱法已被用于检测化学物质与受体之间的结合事件和测量结合选择性。XRF 还可用于估算化学品的治疗指数。XRF 还可用于估算化学品的治疗指数、估算化学品与化学类似物的结合选择性、测量蛋白质的翻译后修饰以及药物生产。
• [EN] 2-ISOPROPYLMALATE SYNTHASE, ENGINEERED BACTERIA OF SAME, AND APPLICATIONS THEREOF<br/>[FR] 2-ISOPROPYLMALATE SYNTHASE, BACTÉRIES GÉNÉTIQUEMENT MODIFIÉES ASSOCIÉES, ET LEURS APPLICATIONS<br/>[ZH] 一种2-异丙基苹果酸合成酶及其工程菌与应用
  申请人：TIANJIN UNIV OF SCIENCE AND TECHNOLOGY

  公开号：WO2021037190A1

  公开（公告）日：2021-03-04

  提供一种2-异丙基苹果酸合成酶及生产L-亮氨酸的基因工程菌及其应用，属于代谢工程领域。所述基因工程菌是通过在宿主细胞中过表达解除L-亮氨酸反馈抑制异丙基苹果酸合成酶编码基因leuA M、解除L-异亮氨酸反馈抑制乙酰乳酸合酶编码基因ilvBN M、3-异丙基苹果酸脱氢酶编码基因leuB、3-异丙基苹果酸脱水酶编码基因leuCD获得。所述的L-亮氨酸基因工程菌无营养缺陷、生长快、发酵周期短、产量高、转化率高。