L-lysine trifluoroacetate | 79360-16-0

• 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: L-lysine trifluoroacetate
• 英文别名: l-Lysine-trifluoroacetate；(2S)-2,6-diaminohexanoic acid;2,2,2-trifluoroacetic acid
• CAS: 79360-16-0
• 化学式: C₂HF₃O₂*C₆H₁₄N₂O₂
• 分子量: 260.213
• InChiKey: GBGCQZQJCOQSLB-JEDNCBNOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.16
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  127
• 氢给体数：
  4
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  L-lysine trifluoroacetate 以 氨 、 水 为溶剂， 反应 15.0h， 生成 L-赖氨酸
  参考文献：
  名称：

  Method of Preparing Grafted Polylysine Dendrimers

  摘要：

  使用活性α-氨基酸单体制备水疏性沉淀态聚肽，其中聚肽是由上述活性α-氨基酸单体在水溶剂中聚合而成，并可在溶剂中重新溶解。

  公开号：

  US20080206183A1
• 作为产物：
  描述：

  (S)-2,6-二叔丁氧羰基氨基己酸 在 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 甲醇 、 二氯甲烷 、 乙腈 为溶剂， 反应 15.0h， 生成 L-lysine trifluoroacetate
  参考文献：
  名称：

  可光裂解的抗菌肽模拟物可排除抗生素耐药性†

  摘要：

  方便地构建了具有赖氨酸基亲水基团，烷基链基疏水基团和邻硝基苄基基团的阳离子两亲物，它们对革兰氏阳性菌和革兰氏阴性菌均显示出依赖烷基链的抗菌活性，对哺乳动物细胞的低细胞毒性和可紫外线裂解的特性，代表了一种新型的无环境累积的抗菌肽模拟物。

  DOI：

  10.1039/c8nj00015h

文献信息

• Macromolecules
  申请人：Owen David

  公开号：US09744246B2

  公开（公告）日：2017-08-29

  The present invention relates to a macromolecule comprising a dendrimer having surface amino groups to which at least two different terminal groups are attached including a pharmaceutically active agent and a pharmacokinetic modifying agent, the pharmaceutically active agent comprising a hydroxyl group and being attached to the surface amino group of the dendrimer through a diacid linker. Pharmaceutical compositions comprising the macromolecules and methods of treatment using the macromolecules are also described.

  本发明涉及一种大分子，包括具有表面氨基团的树枝状聚合物，至少连接有两种不同末端基团，包括药用活性剂和药代动力学修饰剂，所述药用活性剂包括一个羟基，并通过二酸链连接剂连接到树枝状聚合物的表面氨基团上。还描述了包含这种大分子的药物组合物和使用这种大分子进行治疗的方法。
• CONTROLLED MOLECULAR WEIGHT AMINO ACID POLYMERS HAVING FUNCTIONALIZABLE BACKBONES AND END GROUPS AND PROCESSES FOR PREPARING THE SAME
  申请人：Scholz Carmen

  公开号：US20090131589A1

  公开（公告）日：2009-05-21

  The present disclosure relates to processes for preparing metal-free, mono-dispersed polymers of amino acids. The polymers include homopolymers, random copolypeptides, block copolypeptides, block copolymers with at least one peptidyl block, grafted copolypeptides, and polypetidyl dendrimers. The disclosed process does not make use of a heavy metal catalyst, inter alia, copper or nickel containing reagents. The disclosed process encompasses a “living polymerization” such that the growth of each polymer chain is not truncated or otherwise halted by undesirable side reactions or limitations due to the length or size of the growing polymer chain, provides amino acid comprising polymers having a narrow polydispersity, is conducted at lower temperatures, and avoids the premature secondary folding that inhibits the formation of polymers having a low polydispersity index. This abstract is intended to provide key words and search terms for use in searching patent and patent application data bases and is not intended to limit the subject matter of the disclosure.

  本公开涉及制备无金属、单分散氨基酸聚合物的工艺。所述聚合物包括同聚物、随机共聚肽、嵌段共聚肽、至少具有一个肽基块的嵌段共聚物、接枝共聚肽和聚肽树状体。所述工艺不使用重金属催化剂，包括铜或镍含量试剂等。所述工艺包括“活性聚合”，使得每个聚合物链的生长不受不良副反应或由于聚合物链的长度或大小而受到限制的截断，提供具有狭窄聚集度的氨基酸聚合物，以较低的温度进行，并避免抑制具有低聚集度指数的聚合物形成的过早二级折叠。本摘要旨在提供用于搜索专利和专利申请数据库的关键词和搜索术语，不旨在限制本公开的主题。
• Cell-specific glycopeptide ligands
  申请人：Merck & Co., Inc.

  公开号：EP0063373A1

  公开（公告）日：1982-10-27

  Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides include e.g. N2-N2, N6-bis[3-(a-D-mannopyranosylthio)propionyl]-L-lysyl} -N6- [3-(a-D-mannopyranosylthiolpropionyl]-L-lysine (5). Those compounds are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release.

  由糖和氨基酸或肽的共轭物组成的细胞特异性配体是由氨基酸（如鸟氨酸、赖氨酸）、肽（如二赖氨酸、二鸟氨酸或低聚赖氨酸）和具有活性官能团并受适当阻断基团保护的精选糖合成的。这类糖肽包括如 N2-N2，N6-双[3-（a-D-吡喃甘露糖硫基）丙酰基]-L-赖氨酸}-N6-[3-（a-D-吡喃甘露糖硫基）丙酰基]-L-赖氨酸（5）。这些化合物是有用的组织特异性物质，当通过可代谢或可水解的连接与生物活性物质结合时，可将这些生物活性物质输送到选定的部位。通过这种方式，地塞米松等抗炎药物通过可代谢或可水解连接，在给患有炎症疾病的动物用药时，可将药物带到炎症部位进行细胞内释放。
• Cell-specific ligands for selective drug delivery to tissues and organs
  作者：Mitree M. Ponpipom、Robert L. Bugianesi、James C. Robbins、T. W. Doebber、T. Y. Shen

  DOI：10.1021/jm00144a004

  日期：1981.12

  Various numbers of D-mannose residues have been attached via spacer arms to lysine, dilysine, and oligolysine backbones. These D-mannosyl peptide analogues were found to be potent competitive inhibitors of the uptake of 125I-labeled D-mannose-bovine serum albumin conjugate by rat alveolar macrophages. The inhibitory potency of these synthetic ligands increased with increasing number of carbohydrate moieties. The chirality of the peptide backbone did not appear to play a major role in binding, whereas variations of the length and linkage of the spacer arm notably affected the inhibitory activities. The saccharide specificity of the macrophage receptor was demonstrated by the inactivity of the corresponding D-galactosyl peptide analogues. The L-fucosyl peptide derivative was only weakly active. The trimannosyldilysine ligand (KI = 3.9 microM) and its analogues are potentially useful in selective delivery of therapeutic agents to macrophages.
• Synthesis of an amphiphilic tetraantennary mannosyl conjugate and incorporation into liposome carriers
  作者：Socorro Espuelas、Philippe Haller、Francis Schuber、Benoı̂t Frisch

  DOI：10.1016/s0960-894x(03)00472-4

  日期：2003.8

  We have synthesized a novel conjugate (Man(4)K(3)DOG) composed of a tetramannosyl head group connected, via a polyethylene glycol spacer, to a lipid moiety. This amphiphilic molecule was easily incorporated into the bilayers of liposomes. As expected from the clustering effect, such multivalent mannose residues when exposed on the surface of the vesicles showed much higher binding affinity for Concanavalin A than their monomannosyl analogue. Mannosylated liposomes prepared with the tetravalent antenna could be promising carriers for e.g., loading dendritic cells with antigens for vaccination purposes. (C) 2003 Elsevier Ltd. All rights reserved.