glycine-N-(4,6-dimethylpyridin-2-yl)amide | 162103-62-0

• 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: glycine-N-(4,6-dimethylpyridin-2-yl)amide
• 英文别名: 2-amino-N-(4,6-dimethylpyridin-2-yl)acetamide
• CAS: 162103-62-0
• 化学式: C₉H₁₃N₃O
• 分子量: 179.222
• InChiKey: SYYYIEKDESZGBV-UHFFFAOYSA-N

物化性质

• 沸点：
  368.0±42.0 °C(Predicted)
• 密度：
  1.179±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  68
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  glycine-N-(4,6-dimethylpyridin-2-yl)amide 在 palladium on activated charcoal 氢气 、 N,N'-羰基二咪唑 作用下， 以 甲醇 为溶剂， 25.0 ℃ 、101.33 kPa 条件下， 生成 L-alanyl-glycine-N-(4,6-dimethylpyridin-2-yl)amide
  参考文献：
  名称：

  6-Amino-2,4-lutidine carboxamides: α-aminoamide derivatives as systemic and topical inflammation inhibitors

  摘要：

  The development of new potential anti-inflammatory compounds resulting from the incorporation of alpha-aminoacid residues into 6-amino-2,3-lutidine afforded (N-protected) aminoamides with interesting inhibitory activity. Out of 28 tested compounds, 10 (5a, 5b, 7d, 8a, 8b, 8d, 10a, 11b, 12a and 12b) exerted potent (> 90%) inhibition in the carrageenan foot edema (CFE) rat model after oral administration of 0.4 mmol kg(-1). Except for Cbz-glycyl, Cbz-alanyl, Fmoc-valyl and Cbz-alanyl-glycyl derivatives (5a, 5b, 7d and 11b), N-deprotection afforded more active compounds. Introduction of a glycyl residue in the previously studied highly active 3-fluorobenzamide 2, which led to 10a, maintained potent peripheral edema inhibition but had a detrimental effect in the acute TPA-induced mouse ear-swelling model. Glycylglycinamide 12a, which had an ID50 of 9.0 mg kg(-1) in the CFE test, appeared to be the most efficient compound tested in this new series of non-carboxylic nonsteroidal anti-inflammatory drugs. Glycinamide 8a, although less potent in the same assay (14.3 mg kg(-1)), exerted a significant inhibitory effect in acute and chronic ear-swelling tests after topical application of 3 mg/ear. (C) Elsevier, Paris.

  DOI：

  10.1016/s0223-5234(98)80022-6
• 作为产物：
  描述：

  2-氨基-4,6-二甲基吡啶 在 palladium on activated charcoal 氢气 作用下， 以 四氢呋喃 为溶剂， 25.0 ℃ 、101.33 kPa 条件下， 反应 10.0h， 生成 glycine-N-(4,6-dimethylpyridin-2-yl)amide
  参考文献：
  名称：

  Synthesis and hypolipidemic activity of N-pyridinyl borodipeptidylamides

  摘要：

  A series of borodipeptide derivatives 7-9, which contain a 6-amino-2,4-dimethylpyridine moiety, was prepared in 3 steps. They were evaluated as hypolipidemic agents in rodents at 20 mg/kg per day. The methioninamide and phenylalaninamide derivatives were the most potent compounds demonstrating hypocholesterolemic and hypotriglyceridemic activities in rats. After 14 days, the activity of these compounds was superior to that of clofibrate, at a dose of 200 mg/kg per day.

  DOI：

  10.1016/0223-5234(94)90111-2

文献信息

• Alpha-amino acid compounds
  申请人：Adir Et Compagnie

  公开号：US05585390A1

  公开（公告）日：1996-12-17

  Compounds of the general formula: ##STR1## wherein m, X, Y, A, R.sub.2 and R.sub.3 are defined in the description, and medicaments containing the same.

  通式为：##STR1## 其中m、X、Y、A、R.sub.2和R.sub.3在描述中有定义的化合物，以及含有该化合物的药物。
• Nouveaux dérivés d'alpha amino acides leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
  申请人：ADIR ET COMPAGNIE

  公开号：EP0632026A1

  公开（公告）日：1995-01-04

  Composés de formule générale : dans laquelle m, X, Y, A, R₂ et R₃ sont définis dans la description. Médicaments.

  通式......的化合物 其中 m、X、Y、A、R₂ 和 R₃ 如说明中所定义。 药物。
• Synthesis and hypolipidemic activity of N-pyridinyl borodipeptidylamides
  作者：M DUFLOS、S ROBERTPIESSARD、J ROBERT、M ANDRIAMANAMIHAJA、G LEBAUT、B ROBERT、F MAINARD

  DOI：10.1016/0223-5234(94)90111-2

  日期：——

  A series of borodipeptide derivatives 7-9, which contain a 6-amino-2,4-dimethylpyridine moiety, was prepared in 3 steps. They were evaluated as hypolipidemic agents in rodents at 20 mg/kg per day. The methioninamide and phenylalaninamide derivatives were the most potent compounds demonstrating hypocholesterolemic and hypotriglyceridemic activities in rats. After 14 days, the activity of these compounds was superior to that of clofibrate, at a dose of 200 mg/kg per day.
• US5470864A
  申请人：——

  公开号：US5470864A

  公开（公告）日：1995-11-28
• US5585390A
  申请人：——

  公开号：US5585390A

  公开（公告）日：1996-12-17