| 87480-47-5

• 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
• CAS: 87480-47-5
• 化学式: C₁₂H₂₄N₂O₇
• 分子量: 308.332
• InChiKey: OGNUOWCDUQCLHO-VPJKUYQRSA-N

物化性质

• 沸点：
  709.2±60.0 °C(Predicted)
• 密度：
  1.48±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.92
• 重原子数：
  21.0
• 可旋转键数：
  11.0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  176.83
• 氢给体数：
  7.0
• 氢受体数：
  8.0

反应信息

• 作为产物：
  描述：

  D-甘露糖 、 L-赖氨酸盐酸盐 在 sodium hydroxide 、 溶剂黄146 作用下， 反应 24.0h， 生成
  参考文献：
  名称：

  Microspheres based on mannosylated lysine-co-sodium alginate for macrophage-specific delivery of isoniazid

  摘要：

  The present investigation reports coupling of epsilon- and alpha-amino groups of lysine (LS) with mannose (m-LS) and sodium alginate (SA), respectively, to reduce its toxicity. Prepared conjugate, m-LS-co-SA, was characterized through infra-red spectroscopy and differential scanning calorimetry. Cell viability studies were undertaken to assess the safety profile of the prepared conjugate. Microspheres, based on the conjugate, were prepared using spray drying technique and studied for targeting of isoniazid to alveolar macrophages (AMs). Pharmacokinetic studies of the optimized formulation batch were performed in Charles Foster rats.Infra-red spectral data of the synthesized conjugate were in agreement to the presumptive sequence of the conjugation process. Dispersibility, thermal stability and safety of the conjugate were conducive to its biomedical application. Microspheres, formulated from the conjugate, were of uniform size and offered satisfactory drug loading efficiency and in vitro release characteristics. X-ray diffraction studies established that drug was entrapped within the microspheres rather than being adsorbed on to the surface. Pharmacokinetic studies revealed that the conjugate could be a potential vehicle towards both active targeting of isoniazid to AMs and controlling its release rate. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.carbpol.2011.09.056

文献信息

• Peptidotriazoles with antimicrobial activity against bacterial and fungal plant pathogens
  作者：Imma Güell、Lluís Micaló、Laura Cano、Esther Badosa、Rafael Ferre、Emilio Montesinos、Eduard Bardají、Lidia Feliu、Marta Planas

  DOI：10.1016/j.peptides.2011.12.003

  日期：2012.1

  We designed and prepared peptidotriazoles based on the antimicrobial peptide BP100 (LysLysLeuPheLysLysIleLeuLysTyrLeu-NH2) by introducing a triazole ring in the peptide backbone or onto the side chain of a selected residue. These compounds were screened for their in vitro growth inhibition of bacterial and fungal phytopathogens, and for their cytotoxic effects on eukaryotic cells and tobacco leaves. Their proteolytic susceptibility was also analyzed. The antibacterial activity and the hemolysis were influenced by the amino acid that was modified with the triazole as well as by the absence of presence of a substituent in this heterocyclic ring. We identified sequences active against the bacteria Xanthomonas axonopodis pv. vesicatoria, Erwinia amylovora, Pseudomonas syringae pv. syringae (MIC of 1.6-12.5 mu M), and against the fungi Fusarium oxysporum (MIC < 6.2-12.5 mu M) with low hemolytic activity (0-23% at 50 mu M), high stability to protease digestion and no phytotoxicity. These peptidotriazoles constitute good candidates to design new antimicrobial agents. (C) 2011 Elsevier Inc. All rights reserved.