H-β-Ala-OFm

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: H-β-Ala-OFm
• 英文别名: 9H-fluoren-9-ylmethyl 3-aminopropanoate
• 化学式: C₁₇H₁₇NO₂
• 分子量: 267.327
• InChiKey: RVGIHWRZFKEMJU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  52.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  FMOC-beta-丙氨酸 、 H-β-Ala-OFm 、 glutaric acid mono(fluoren-9-yl)methyl ester 生成 3-[3-(4-{2-[2-(9H-Fluoren-9-ylmethoxycarbonyl)-ethylcarbamoyl]-ethylcarbamoyl}-butyrylamino)-propionylamino]-propionic acid
  参考文献：
  名称：

  Multivalent Drug Design. Synthesis and In Vitro Analysis of an Array of Vancomycin Dimers

  摘要：

  The design, synthesis, and in vitro microbiological analysis of an array of forty covalently linked vancomycin dinners are reported. This work was undertaken to systematically probe the impact of linkage orientation and linker length on biological activity against susceptible and drug-resistant Gram-positive pathogens. To prepare the array, monomeric vancomycin synthons were linked through four distinct positions of the glycopeptide (C-terminus (C), N-terminus (N), vancosamine residue (V), and resorcinol ring (R)) in 10 unique pairwise combinations. Amphiphilic, peptide-based linkers of four different lengths (111, 19, 27, and 43 total atoms) were employed. Both linkage orientation and linker length were found to affect in vitro antibacterial potency. The V-V series displayed the greatest potency against vancomycin-susceptible organisms and vancomycin-resistant Enterococcus faecalis (VRE) of VanB phenotype, while the C-C, C-V, and V-R series displayed the most promising broad-spectrum activity that included VRE of VanA phenotype. Dimers bearing the shortest linkers were in all cases preferred for activity against VRE. The effects of linkage orientation and linker length on in vitro potency were not uniform; for example, (1) no single compound displayed activity that was superior against all test organisms to that of vancomycin or the other dimers, (2) linker length effects varied with test organism, and (3) whereas one-half of the dimers were more potent than vancomycin against methicillin-susceptible Staphylococcus aureus (MSSA), only one dimer was more potent against methicillin-resistant S. aureus (MRSA) and glycopeptide-intermediate susceptible S. aureus (GISA). In interpreting the results, we have considered the potential roles of multivalency and of other phenomena.

  DOI：

  10.1021/ja021273s

文献信息

• Transmetalation Methods for the Synthesis of PET and SPECT Imaging Agents
  申请人：Schmitthenner Hans F.

  公开号：US20160251378A1

  公开（公告）日：2016-09-01

  A process for the preparation of a radionuclide imaging agent includes providing an imaging agent including a chelated place-holder metal; loading the imaging agent onto an acid stable stationary phase; replacing the chelated place-holder metal of the imaging agent loaded on the stationary phase with a replacement radioactive metal under mild reaction conditions; and eluting the imaging agent including the chelated replacement radioactive metal from the stationary phase to provide a radionuclide imaging agent suitable for positron emission tomography (PET) or single-photon emission computed tomography (SPECT). The imaging agent can include a targeting agent that is directly conjugated to the imaging agent or by means of a linker. The process may also apply to other metals that are non-radioactive but used as diluent metals or other metals that are strongly bound to DOTA.

  制备放射性核素成像剂的过程包括提供一个包含螯合占位金属的成像剂；将成像剂加载到酸稳定的固定相上；在温和反应条件下用替代放射性金属替换固定相上加载的成像剂的螯合占位金属；并从固定相中淋洗包含螯合替代放射性金属的成像剂，以提供适用于正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）的放射性核素成像剂。该成像剂可以包括直接共轭到成像剂或通过连接剂共轭到成像剂的靶向剂。该过程也可适用于其他非放射性金属，但用作稀释剂金属或其他强结合到DOTA的金属。
• Vectors for dna delivery
  申请人：——

  公开号：US20030207400A1

  公开（公告）日：2003-11-06

  The present invention pertains to novel products suitable for use as gene delivery systems in which nucleic acid is linked to a ligand in order to facilitate delivery of the nucleic acid to a target cell or sub-cellular compartment via uptake of the ligand. More particularly, the present invention pertains to vectors comprising: (a) a double stranded DNA (dsDNA) having at least one target sequence; and, (b) a chimeric molecule comprising: (i) a sequence specific polyamide (SSP) moiety bound non-covalently to said target sequence; and, (ii) a ligand moiety linked covalently to said sequence specific polyamide. The present invention also pertains to compositions comprising such chimeric molecules and vectors; methods for making such chimeric molecules and vectors; and methods of using such chimeric molecules and vectors, e.g., to deliver nucleic acid vectors to cells or sub-cellular compartments.

  本发明涉及新型产品，适用于用作基因传递系统，其中核酸与配基连接，以便通过配基的摄取促进核酸传递到目标细胞或亚细胞区域。更具体地，本发明涉及包括：（a）至少具有一个目标序列的双链DNA（dsDNA）；以及（b）包括的嵌合分子：（i）与所述目标序列非共价结合的序列特异性聚酰胺（SSP）基团；以及（ii）与所述序列特异性聚酰胺共价连接的配基基团。本发明还涉及包含这种嵌合分子和向量的组合物；制备这种嵌合分子和向量的方法；以及使用这种嵌合分子和向量的方法，例如将核酸向量传递到细胞或亚细胞区域。
• VECTORS FOR DNA DELIVERY
  申请人：ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A.

  公开号：EP1290198A2

  公开（公告）日：2003-03-12
• Modular Imaging Agents Containing Amino Acids and Peptides
  申请人：Schmitthenner Hans F.

  公开号：US20170246326A1

  公开（公告）日：2017-08-31

  Targeted molecular imaging agents (TMIAs) are derived from coupling together pre-formed amino acids with imaging agents attached to their side chains. These peptide-based imaging agents may be synthesized from a single or multiple preformed amino acids containing multi-modal, multi-chelated metal, multi-dye imaging agents, or combinations of these, on the side chains of resultant peptides. These imaging amino acids or peptides may be conjugated directly, or activated, or attached to linkers to which targeting groups, such as peptides, proteins, antibodies, aptamers, or small molecule inhibitors, may be conjugated in the final steps of the synthesis to form a wide variety of TMIAs.
• [EN] VECTORS FOR DNA DELIVERY<br/>[FR] VECTEURS POUR LIBERATION D'ADN
  申请人：ANGELETTI P IST RICHERCHE BIO

  公开号：WO2001088160A2

  公开（公告）日：2001-11-22

  The present invention pertains to novel products suitable for use as gene delivery systems in which nucleic acid is linked to a ligand in order to facilitate delivery of the nucleic acid to a target cell or sub-cellular compartment via uptake of the ligand. More particularly, the present invention pertains to vectors comprising: (a) a double stranded DNA (dsDNA) having at least one target sequence; and, (b) a chimeric molecule comprising: (i) a sequence specific polyamide (SSP) moiety bound non-covalently to said target sequence; and, (ii) a ligand moiety linked covalently to said sequence specific polyamide. The present invention also pertains to compositions comprising such chimeric molecules and vectors; methods for making such chimeric molecules and vectors; and methods of using such chimeric molecules and vectors, e.g., to deliver nucleic acid vectors to cells or sub-cellular compartments.