ampicillin hydrochloride | 40688-84-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: ampicillin hydrochloride
• 英文别名: (2S,5R,6R)-6-[[(2R)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid;hydrochloride
• CAS: 40688-84-4
• 化学式: C₁₆H₁₉N₃O₄S*ClH
• 分子量: 385.871
• InChiKey: DRLJIPQOBJCEET-YWUHCJSESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.74
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  138
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  ampicillin hydrochloride 、 4-芘甲醛 在 三乙胺 作用下， 以 甲醇 、 水 为溶剂， 反应 0.5h， 生成
  参考文献：
  名称：

  标记辅助激光解吸/电离质谱（LA-LDI-MS）：使用醛检测生物胺，氨基酸和肽†

  摘要：

  标记辅助激光解吸/电离（LA-LDI）技术最近已应用于通过飞行时间（TOF）质谱测量来检测小分子。通过排除外部基质，质谱变得更加干净，没有基质相关的峰和噪声。对应于分析物和标记物之间形成的化合物/复合物的峰通常在光谱中可见。在本文中，我们报告了一种基于LA-LDI质谱法的胺检测方法，其中包括使用1-py甲醛作为LDI标签的生物样品中普遍存在的胺，如生物胺，氨基酸，二肽和三肽。

  DOI：

  10.1039/c5ra20678b

文献信息

• NOVEL SUSTAINED RELEASE DOSAGE FORM
  申请人：Pilgaonkar Pratibha S.

  公开号：US20090053310A1

  公开（公告）日：2009-02-26

  The novel sustained release dosage form comprising an active agent and a combination of a non-swelling pH dependent release retardant and a non swelling pH independent release retardant polymer which provides pH-independent drug release for a considerable period of time after administration.

  这段话的意思是：该小说维持释放速度的剂型包括一种活性剂和非肿胀的pH依赖性缓释剂和非肿胀的pH独立性缓释剂聚合物的组合，该组合在给药后相当长一段时间内提供pH独立的药物释放。
• BIOACTIVE POLYMER PRODUCT
  申请人：EBARA CORPORATION

  公开号：EP0940144A1

  公开（公告）日：1999-09-08

  A biologically active polymer product having a biologically active compound moiety immobilized to a polymer substrate through a covalent bond. The biologically active compound moiety such as an antibiotic exerts selective biological activity while being covalently bonded to the polymer substrate. A biologically active polymer product in which two or more biologically active compound moietys are linked to a polymer substrate through a graft chain or a pendant chain.

  一种生物活性聚合物产品，其生物活性化合物分子通过共价键固定在聚合物基底上。生物活性化合物分子（如抗生素）在与聚合物基质共价键结合的同时，可发挥选择性生物活性。生物活性聚合物产品，其中两个或多个生物活性化合物分子通过接枝链或悬垂链与聚合物基底相连。
• Preparation of beta-lactam antibiotics in the presence of urea or amide
  申请人：GIST-BROCADES B.V.

  公开号：EP0953569A1

  公开（公告）日：1999-11-03

  A process for the preparation of β-lactam compounds has been described wherein before the addition of a base, urea or derivatives thereof and/or amide or derivatives has been added to (a) before an acid hydrolysis of the Dane salt coupling reaction mixture resulting from acylation of 6-amino-penicillanic acid, 7-amino-cephalosporanic acid or 7-amino-3'-desacetoxycephalosporanic acid and derivatives thereof at low temperature or to (b) a solution obtained by the addition of an acid to the crude β-lactam antibiotic compound in water and/or one or more organic solvents.

  描述了一种制备β-内酰胺化合物的工艺，其中在加入碱之前，已将脲或其衍生物和/或酰胺或其衍生物加入到(a)6-氨基-青霉烷酸酰化产生的达内盐偶联反应混合物的酸水解之前，或(b)在低温下加入7-氨基-头孢烷酸或7-氨基-3'-双乙酰氧基头孢烷酸及其衍生物得到的溶液中、7-amino-cephalosporanic acid 或 7-amino-3'-desacetoxycephalosporanic acid 及其衍生物，或 (b) 在水中和/或一种或多种有机溶剂中向粗制 β-内酰胺抗生素化合物中加入酸而得到的溶液。
• STABLE MEDICINAL COMPOSITIONS FOR ORAL USE
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP1205190A1

  公开（公告）日：2002-05-15

  The present invention is to provide a stable pharmaceutical composition for oral use and preparation thereof in which changes are prevented in drug release during storage even under the exposure to light, by adding yellow ferric oxide and/or red ferric oxide in a matrix type sustained-release preparation containing a drug, a hydrophilic base, and polyethylene oxide. The present invention is to further provide a method for preventing changes in drug release during storage under the exposure to light in a matrix type sustained-release preparation containing a drug, a hydrophilic base, and polyethylene oxide. The quality assurance period of the product can be prolonged and the product value can be improved by the present invention.

  本发明旨在提供一种稳定的口服药物组合物及其制备方法，通过在含有药物、亲水性基质和聚氧化乙烯的基质型缓释制剂中添加黄色氧化铁和/或红色氧化铁，即使在光照下也能防止药物释放在储存过程中发生变化。本发明进一步提供一种方法，用于防止含有药物、亲水性基质和聚氧化乙烯的基质型缓释制剂在光照下储存期间药物释放量发生变化。通过本发明可以延长产品的质量保证期，提高产品价值。
• Peptide-based method for monitoring gene expression in a host cell
  申请人：Friedrich-Alexander-Universität Erlangen-Nürnberg

  公开号：EP1580273A1

  公开（公告）日：2005-09-28

  The present invention relates a method for monitoring the expression level of a gene in a host cell by modulating the activity of a regulatory biomolecule, comprising the steps of: (a) transforming a cell expressing a regulatory biomolecule with a nucleic acid molecule comprising an open reading frame encoding an interaction partner of said biomolecule in expressible form, wherein (i) said regulatory biomolecule is either a nucleic acid binding molecule that effects its regulatory activity upon binding or an allosterically controlled ribonucleic acid molecule; and (ii) the interaction partner of the biomolecule is encoded by a nucleic acid molecule comprising: (1) a nucleic acid sequence encoding a tagged (poly)peptide, or (2) a nucleic acid sequence encoding a tagged (poly)peptide or a peptide tag, a selectable marker gene and additional nucleotide sequences for site specific, in-frame integration of said nucleic acid molecule into the coding sequence of at least one host (poly)peptide of interest, wherein said tag comprises the interacting residues of the interaction partner and (b) assessing the expression level of the gene. Furthermore, the present invention relates to a method of producing and/or selecting a compound capable of modulating the activity of a nucleic acid binding protein comprising the steps of: (a) conducting a selection of compounds with the nucleic acid binding target protein under conditions allowing an interaction of the compound and the nucleic acid binding protein; (b) removing unspecifically bound compounds; (c) detecting specific binding of compounds to the nucleic acid binding target protein; (d) expressing in a cell, the nucleic acid binding protein and providing in trans the coding sequence of at least one indicator gene, wherein said coding sequence is under control of the target sequence of the nucleic acid binding protein; (e) adding a candidate compound to the cell of step (d); (f) determining the amount or activity of the indicator protein, wherein a reduced or increased amount of indicator protein is indicative of compounds, capable of modulating the activity of the nucleic acid binding protein; (g) selecting compounds capable of modulating the activity of the nucleic acid binding protein. Moreover, the present invention relates to nucleic acid molecules, polypeptides, expression vectors, host cells, ensembles of host cells and a non-human animal comprising said host cells. Finally, the present invention relates to a kit comprising the nucleic acid molecule, the (poly)peptide, the vector, the host cell or the ensemble of host cells of the present invention in one or more containers.

  本发明涉及一种通过调节调控生物分子的活性来监测宿主细胞中基因表达水平的方法，包括以下步骤：(a) 用包含开放阅读框的核酸分子转化表达调控生物大分子的细胞，该开放阅读框以可表达的形式编码所述生物大分子的相互作用伙伴，其中(i) 所述调控生物大分子是一种核酸结合分子，结合后可影响其调控活性，或者是一种异位控制的核糖核酸分子；以及(ii) 生物大分子的相互作用伙伴由核酸分子编码，该核酸分子包含：(1)编码标记(多)肽的核酸序列，或(2)编码标记(多)肽或肽标签的核酸序列、可选择标记基因和附加核苷酸序列，用于将所述核酸分子定点、框内整合到至少一种感兴趣的宿主(多)肽的编码序列中，其中所述标签包括相互作用伙伴的相互作用残基；以及(b)评估基因的表达水平。此外，本发明还涉及一种生产和/或筛选能够调节核酸结合蛋白活性的化合物的方法，包括以下步骤：(a) 在允许化合物与核酸结合蛋白相互作用的条件下，对与核酸结合靶蛋白结合的化合物进行筛选； (b) 去除非特异性结合的化合物； (c) 检测化合物与核酸结合靶蛋白的特异性结合； (d) 在细胞中表达核酸结合蛋白，并反式提供至少一个指示基因的编码序列，其中所述编码序列受核酸结合蛋白靶序列的控制；(e) 向步骤(d)的细胞中加入候选化合物； (f) 确定指示蛋白的量或活性，其中指示蛋白量的减少或增加表明化合物能够调节核酸结合蛋白的活性； (g) 选择能够调节核酸结合蛋白活性的化合物。此外，本发明还涉及核酸分子、多肽、表达载体、宿主细胞、宿主细胞组合以及包含所述宿主细胞的非人类动物。最后，本发明涉及一种试剂盒，该试剂盒包含本发明的核酸分子、（多）肽、载体、宿主细胞或宿主细胞组合，装在一个或多个容器中。