3-(2-methyl-1H-imidazol-1-yl)propanehydrazide | 852378-49-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-(2-methyl-1H-imidazol-1-yl)propanehydrazide
• 英文别名: 3-(2-Methyl-1h-imidazol-1-yl)propiohydrazide；3-(2-methylimidazol-1-yl)propanehydrazide
• CAS: 852378-49-5
• 化学式: C₇H₁₂N₄O
• 分子量: 168.198
• InChiKey: MXADUISOFDKAFE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  72.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(2-methyl-1H-imidazol-1-yl)propanehydrazide 、 2-羟基-1-萘甲醛 在 溶剂黄146 作用下， 以 乙醇 为溶剂， 反应 6.0h， 以31%的产率得到N'-[(E)-(2-hydroxynaphthalen-1-yl)methylidene]-3-(2-methyl-1H-imidazol-1-yl)propanehydrazide
  参考文献：
  名称：

  Structure–Activity Studies of Divin: An Inhibitor of Bacterial Cell Division

  摘要：

  We describe the synthesis and structure activity relationship (SAR) studies of divin, a small molecule that blocks bacterial division by perturbing the assembly of proteins at the site of cell septation. The bacteriostatic mechanism of action of divin is distinct from other reported inhibitors of bacterial cell division and provides an opportunity for assessing the therapeutic value of a new class of antimicrobial agents. We demonstrate a convenient synthetic route to divin and its analogues, and describe compounds with a 10-fold increase in solubility and a 4-fold improvement in potency. Divin analogues produce a phenotype that is identical to divin, suggesting that their biological activity comes from a similar mechanism of action. Our studies indicate that the 2-hydroxynaphthalenyl hydrazide portion of divin is essential for its activity and that alterations and substitution to the benzimidazole ring can increase its potency. The SAR study provides a critical opportunity to isolate drug resistant mutants and synthesize photoaffinity probes to determine the cellular target and biomolecular mechanism of divin.

  DOI：

  10.1021/ml400234x
• 作为产物：
  描述：

  3-(2-methyl-imidazol-1-yl)-propionic acid methyl ester 在 一水合肼 作用下， 以 甲醇 为溶剂， 反应 16.0h， 以94%的产率得到3-(2-methyl-1H-imidazol-1-yl)propanehydrazide
  参考文献：
  名称：

  Structure–Activity Studies of Divin: An Inhibitor of Bacterial Cell Division

  摘要：

  We describe the synthesis and structure activity relationship (SAR) studies of divin, a small molecule that blocks bacterial division by perturbing the assembly of proteins at the site of cell septation. The bacteriostatic mechanism of action of divin is distinct from other reported inhibitors of bacterial cell division and provides an opportunity for assessing the therapeutic value of a new class of antimicrobial agents. We demonstrate a convenient synthetic route to divin and its analogues, and describe compounds with a 10-fold increase in solubility and a 4-fold improvement in potency. Divin analogues produce a phenotype that is identical to divin, suggesting that their biological activity comes from a similar mechanism of action. Our studies indicate that the 2-hydroxynaphthalenyl hydrazide portion of divin is essential for its activity and that alterations and substitution to the benzimidazole ring can increase its potency. The SAR study provides a critical opportunity to isolate drug resistant mutants and synthesize photoaffinity probes to determine the cellular target and biomolecular mechanism of divin.

  DOI：

  10.1021/ml400234x

文献信息

• POLYACETAL RESIN COMPOSITION
  申请人：Polyplastics Co., Ltd.

  公开号：EP1686156A1

  公开（公告）日：2006-08-02

  A polyacetal resin composition comprises a polyacetal resin and a hetero atom-containing aliphatic carboxylic acid hydrazide. The proportion of the hetero atom-containing aliphatic carboxylic acid hydrazide may be about 0.001 to 20 parts by weight relative to 100 parts by weight of the polyacetal resin. The polyacetal resin composition may further comprise at least one member selected from the group consisting of an antioxidant, a heat stabilizer, a processing stabilizer, a weather (light)-resistant stabilizer, an impact resistance improver, a gloss control agent, an agent for improving sliding property, a coloring agent, and a filler. Such a resin composition improves stability of the polyacetal resin and inhibits formaldehyde emission.

  聚缩醛树脂组合物由聚缩醛树脂和含杂原子的脂肪族羧酸酰肼组成。相对于 100 重量份的聚缩醛树脂，含杂原子的脂肪族羧酸酰肼的比例可为 0.001 至 20 重量份。聚缩醛树脂组合物可进一步包含至少一种选自以下组别的成员：抗氧化剂、热稳定剂、加工稳定剂、耐候（光）稳定剂、抗冲击性改进剂、光泽控制剂、改善滑动性能剂、着色剂和填料。这种树脂组合物可以提高聚缩醛树脂的稳定性，并抑制甲醛释放。
• Polyacetal resin composition
  申请人：Harashina Hatsuhiko

  公开号：US20070054998A1

  公开（公告）日：2007-03-08

  A polyacetal resin composition comprises a polyacetal resin and a hetero atom-containing aliphatic carboxylic acid hydrazide. The proportion of the hetero atom-containing aliphatic carboxylic acid hydrazide may be about 0.001 to 20 parts by weight relative to 100 parts by weight of the polyacetal resin. The polyacetal resin composition may further comprise at least one member selected from the group consisting of an antioxidant, a heat stabilizer, a processing stabilizer, a weather (light)-resistant stabilizer, an impact resistance improver, a gloss control agent, an agent for improving sliding property, a coloring agent, and a filler. Such a resin composition improves stability of the polyacetal resin and inhibits formaldehyde emission.
• US7638565B2
  申请人：——

  公开号：US7638565B2

  公开（公告）日：2009-12-29