[(4S)-4-azaniumyl-5-methoxy-5-oxopentyl]-(diaminomethylidene)azanium;dichloride

• 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: [(4S)-4-azaniumyl-5-methoxy-5-oxopentyl]-(diaminomethylidene)azanium;dichloride
• 化学式: C7H18Cl2N4O2
• mdl: MFCD00038948
• 分子量: 261.15
• InChiKey: XQYZOBNLCUAXLF-XRIGFGBMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.34
• 重原子数：
  15
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.714
• 拓扑面积：
  117
• 氢给体数：
  5
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  [(4S)-4-azaniumyl-5-methoxy-5-oxopentyl]-(diaminomethylidene)azanium;dichloride 、 sodium hydroxide 在 IPHH-2000 、 水 、 碳酸氢钠 、 柠檬酸 作用下， 以 甲醇 为溶剂， 反应 1.5h， 生成 L-精氨酸
  参考文献：
  名称：

  Partial ester of cellulose with nitrogenous carboxylic acid and process for producing the same

  摘要：

  根据本发明，提供了一种新型的氮羧酸酯部分酯化纤维素，该部分酯化物可用作抗菌剂、阻燃剂等，并提供了一种简单方便的制备方法。由该部分酯化物制成的纤维具有耐洗涤的抗菌性和阻燃性。可以通过将氮羧酸酯与纤维素接触并热处理混合物来制备氮羧酸酯部分酯化纤维素。

  公开号：

  US20030027733A1

文献信息

• CATIONIC LIPIDS, METHODS FOR PREPARING THE SAME, AND DELIVERY SYSTEMS HAVING ABILITY TO TRANSITION INTO CELLS COMPRISING THE SAME
  申请人：Park Myung-Ok

  公开号：US20130123485A1

  公开（公告）日：2013-05-16

  The present invention provides cationic lipids, methods for preparing the same, and delivery systems comprising the same. The present invention can provide cationic lipids which enhance the efficiency of intracellular or in vivo delivery of multiple-anionic target compounds such as drugs, anticancer agents, nucleic acids, etc., have no intracellular toxicity, but show increased stability, methods for preparing the same, and delivery systems comprising the same.

  本发明提供了阳离子脂质、其制备方法以及包含该脂质的传递系统。本发明可以提供增强多阴离子靶向化合物（如药物、抗癌剂、核酸等）在细胞内或体内传递效率的阳离子脂质，不具有细胞内毒性，但表现出增加的稳定性，以及其制备方法和包含该脂质的传递系统。
• [EN] GUANIDINE-MODIFIED C-TERMINUS VANCOMYCIN COMPOUNDS, COMPOSITIONS AND METHODS<br/>[FR] COMPOSÉS DE VANCOMYCINE À EXTRÉMITÉ C-TERMINALE MODIFIÉE PAR DE LA GUANIDINE, COMPOSITIONS ET PROCÉDÉS
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2021216323A1

  公开（公告）日：2021-10-28

  A series of vancomycin C-terminus guanidine modifications are disclosed that improve antimicrobial activity, enhance the durability of antimicrobial action against selection or induction of resistance, and provide two synergistic mechanisms of action independent of D-Ala-D-Ala binding that cause inhibition of cell wall biosynthesis, while inducing bacterial cell permeability. A contemplated compound contains two combined peripheral modifications, a (4-chlorobiphenyl)methyl (CBP) and C-terminus guanidine modification, that provide new treatments against not only vancomycin-sensitive, but especially vancomycin- resistant bacteria. The data demonstrate that the synergistic behavior of the peripheral modifications requires the presence of both the CBP and guanidine modifications in a single molecule versus their combined use as an equimolar mixture of singly modified compounds. A prototypical member of the series, G3- CBP-vancomycin (15), exhibits no hemolytic activity, displays no mammalian cell growth inhibition, and possesses improved and especially attractive in vivo pharmacokinetic (PK) properties.

  披露了一系列万古霉素C-末端胍基修饰，可改善抗微生物活性，增强抗微生物作用对抗选择或诱导耐药性的耐久性，并提供两种独立于D-Ala-D-Ala结合的协同作用机制，导致细胞壁生物合成的抑制，同时诱导细菌细胞渗透性。一个可考虑的化合物包含两个组合的外围修饰，即（4-氯联苯）甲基（CBP）和C-末端胍基修饰，可提供新的治疗方法，不仅针对万古霉素敏感的细菌，特别是针对万古霉素耐药菌。数据表明，外围修饰的协同行为需要在单个分子中同时存在CBP和胍基修饰，而不是将它们作为等摩尔混合物的单一修饰化合物的组合使用。该系列的典型成员G3-CBP-万古霉素（15）不表现出溶血活性，不抑制哺乳动物细胞生长，并具有改进的特别有吸引力的体内药物动力学（PK）特性。
• CATIONIC ALPHA-AMINO ACID-CONTAINING BIODEGRADABLE POLYMER GENE TRANSFER COMPOSITIONS
  申请人：Turnell William G.

  公开号：US20090068743A1

  公开（公告）日：2009-03-12

  The invention provides gene transfer compositions using as the gene carrier a biodegradable polymer that contains one or more cationic alpha amino acids, such as arginine or agmatine. The compositions form a tight soluble complex with a poly nucleic acid suitable for transfecting target cells to effect translation of the cargo poly nucleic acid by the target cell. Thus, such compounds are useful both in vitro and in vivo.

  本发明提供了一种基因转移组合物，其中使用可生物降解的聚合物作为基因载体，该聚合物含有一种或多种阳离子α氨基酸，例如精氨酸或脲甲酸。该组合物与适用于转染目标细胞的聚核酸形成紧密的可溶性复合物，以通过目标细胞转化载荷聚核酸的翻译。因此，这些化合物在体外和体内都有用。
• PHENYLSULFAMOYL BENZAMIDE DERIVATIVES AS BRADYKININ ANTAGONISTS
  申请人：Beke Gyula

  公开号：US20100105686A1

  公开（公告）日：2010-04-29

  The present invention relates to new sulfonamide derivatives of formula (I) wherein R 1 -R 8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

  本发明涉及式(I)的新磺酰胺衍生物，其中R1-R8和Z如权利要求中所定义，以及其光学对映体或外消旋体和/或盐和/或水合物和/或溶剂化物，它们是布雷地酮B1的选择性拮抗剂，用于制备这些化合物的方法、包含它们的药理学组合物以及它们在治疗或预防疼痛和炎症状况中的应用。
• New Phenylsulfamoyl Benzamide Derivatives as Bradykinin Antagonists
  申请人：Beke Gyula

  公开号：US20120295910A1

  公开（公告）日：2012-11-22

  The present invention relates to new sulfonamide derivatives of formula (I), wherein R 1 -R 8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

  本发明涉及公式(I)的新磺酰胺衍生物，其中R1-R8和Z如权利要求所定义，以及其光学对映体或混合物和/或盐和/或水合物和/或溶剂化物，它们是缓激肽B1选择性拮抗剂，制备这些化合物的过程，包含它们的药理学组合物以及它们在治疗或预防疼痛和炎症疾病方面的用途。