cephalexin sodium

• 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: cephalexin sodium
• 英文别名: sodium;(2R)-2-amino-N-[(6R,7R)-2-carboxy-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-7-yl]-2-phenylethanimidate
• 化学式: C₁₆H₁₆N₃O₄S*Na
• 分子量: 369.377
• InChiKey: NZDYPHVJLWMLJI-CYJZLJNKSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  -3.89
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  141
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  己基-5-壬基氯 、 cephalexin sodium 在 碳酸氢钠 作用下， 以 水 为溶剂， 反应 1.0h， 以65%的产率得到
  参考文献：
  名称：

  肠杆菌素和沙莫螯合素-β-内酰胺缀合物诱导的细胞形态与尿路致病性大肠杆菌 CFT073 中青霉素结合蛋白的抑制一致

  摘要：

  当已知病原体时，设计和合成针对特定细菌菌株、物种或物种群的窄谱抗生素是治疗细菌感染的一种有前途的策略。在这项工作中，我们报告了四种新的铁载体-β-内酰胺缀合物的合成和评估，其中广谱β-内酰胺抗生素头孢氨苄（Lex）和美罗培南（Mem）共价连接到肠杆菌素（Ent）或二葡萄糖基化Ent（ DGE）通过稳定的聚乙二醇（PEG 3 ）连接体。与母体抗生素相比，这些铁载体-β-内酰胺缀合物对大肠杆菌的最低抑制浓度有所提高。对尿路致病性大肠杆菌CFT073 的摄取研究表明，DGE-β-内酰胺靶向病原体相关的儿茶酚酸铁载体受体 IroN。对含有氨苄青霉素 (Amp)、Lex 和 Mem 的铁载体-β-内酰胺的比较分析表明，DGE-Mem 缀合物具有优势，因为它以 IroN 为靶标，并表现出较低的最低抑制浓度、快速的杀伤动力学以及对丝氨酸 β 的增强的稳定性-内酰胺酶。用铁载体-β-内酰胺缀合物处理的大肠

  DOI：

  10.1039/d0sc04337k
• 作为产物：
  描述：

  头孢氨苄 在 sodium hydroxide 作用下， 以 甲醇 、 乙酸乙酯 为溶剂， 生成 cephalexin sodium
  参考文献：
  名称：

  Methoxymethyl esters of substituted

  摘要：

  式子为 ##STR1## 的化合物中，其中R.sup.1是氢或羟基，是强效的抗菌剂。

  公开号：

  US04125716A1

文献信息

• Substituted N-(1,2-dihydro-2-oxonicotinyl)-cephalexins and
  申请人：Parke, Davis & Company

  公开号：US03948903A1

  公开（公告）日：1976-04-06

  Novel organic amide compounds which are substituted N-(1,2-dihydro-2-oxonicotinyl)-ampicillins, -cephalexins and -cephaloglycins having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid ampicillin, cephalexin or cephaloglycin or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding 1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid or 7-amino-3-methylceph-3-em-4-carboxylic acid or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding N-(1,2-dihydro-2-oxonicotinyl)-2-phenylglycine.

  新型有机酰胺化合物，其为取代的N-(1,2-二氢-2-氧基烟酸基)-氨苄青霉素、头孢氨苄和头孢甘露醇，具有广谱抗菌作用，通过(a)将游离氨基酸氨苄青霉素、头孢氨苄或头孢甘露醇或其酸盐或硅烷衍生物与相应的1,2-二氢-2-氧基烟酸的反应衍生物反应，或(b)将游离氨基酸6-氨基青霉素酸、7-氨基头孢菌素酸或7-氨基-3-甲基头孢-3-烯-4-羧酸或其酸盐或硅烷衍生物与相应的N-(1,2-二氢-2-氧基烟酸基)-2-苯基甘氨酸的反应衍生物反应。
• Eco-friendly and Efficient Synthesis, Characterisation and Antibacterial Studies of Unsymmetrical Bidentate Schiff Bases and their Zn(II) Complexes
  作者：K Srivastava、Anuradha Singh、Suresh Singh

  DOI：10.13005/ojc/300339

  日期：2014.9.26

  A rapid, efficient, clean and environmentally benign exclusive synthesis of Schiff bases as new ligands and their complexes with Zn(II) have been developed using condensation of pyridoxalwith amoxicillin (L1), cephalexin (L2), sulphamethoxazole (L3) and trimethoprim (L4) efficiently in analcoholic suspension medium using alkali catalyst with excellent yields under microwaves irradiation. This method provides several advantages such as environmental friendliness, simple work-up procedure, short reaction times, non-hazardous and excellent yield of products.The results are compared with conventional methods for their yield and reaction time. The Schiff base ligands and the complexes were characterized by micro-analytical, thermo-gravimetric, magnetic and spectroscopic studies.All the Schiff bases were bidentate (NO donor) ligands. All complexes were found to be six co-ordinate dihydrates and ML2[1:2 (metal: ligand) ratio] type. The complexes are coloured and stable in air. All the complexes under investigation possess antibacterial activity. The antibacterial activity showed the following trend:

  一种快速、高效、清洁且环保的希夫碱（作为新配体）及其与Zn(II)的复合物已成功开发，其合成方法为：在无醇悬浮培养基中，使用碱催化剂高效缩合吡哆醛与阿莫西林（L1）、头孢氨苄（L2）、磺胺甲恶唑（L3）和甲氧苄啶（L4），在微波辐射下，可获得极佳的收率。该方法具有诸多优点，例如环保、操作步骤简单、反应时间短、无危险且产品收率高。与传统方法相比，该方法的收率和反应时间更优。通过微量分析、热重分析、磁性和光谱研究，对希夫碱配体和复合物进行了表征。所有希夫碱均为双齿（NO供体）配体。所有复合物均为六配位二水合物，且为ML2[1:2（金属：配体）比]类型。复合物在空气中呈色且稳定。所有被研究的复合物均具有抗菌活性。抗菌活性呈现以下趋势：
• Controlled release oral drug delivery system
  申请人：The Jordanian Pharmaceutical Manufacturing Co.

  公开号：EP1721602A1

  公开（公告）日：2006-11-15

  The invention relates to a molecular ionic complex formed between an acidic pharmaceutical drug or its salt or solvate and glucosamine, chondroitin, hyaluronic acid or heparin or its salts or derivatives. The complex can provide for a liquid oral controlled drug delivery. For example, ibuprofen sodium complex with glucosamine sulfate potassium (GSP) was found to have a zero order controlled drug delivery when given orally to rabbits.

  本发明涉及一种由酸性药物或其盐或溶剂与葡萄糖胺、软骨素、透明质酸或肝素或其盐或衍生物形成的分子离子复合物。该复合物可提供液体口服控制药物释放。例如，发现当将布洛芬钠与硫酸葡萄糖胺钾（GSP）形成复合物后，口服给兔子时具有零级控制药物释放。
• Process for the manufacture of the antibiotic
  申请人：Vitara Chemicals Limited

  公开号：US05908929A1

  公开（公告）日：1999-06-01

  A process for the manufacture of the antibiotic 7-(D-.alpha.-amino-.alpha.-phenylacetamido)-3-methyl-3-cephem-4-carboxylic acid (cephalexin) and pharmaceutically acceptable salts thereof. It consists of reacting an enamine protected potassium salt of D-(-)-.alpha.-phenyl glycine (Dane salt) with an acid chloride in a twin solvent mixture in the presence of a pyridine derived twin catalytic mixture at -20 to -65.degree. C. The resulting mixed anhydride is condensed with an alkyl guanidinium salt solution of 7-amino desacetoxy cephalosporanic acid (7-ADCA) at -10.degree. C. to -65.degree. C. followed by hydrolytic cleavage of the enamine derivative of the resulting compound with an aqueous mineral acid and precipitation of the antibiotic in the presence of an alcohol as co-solvent. If desired the cephalexin is converted into its pharmaceutically acceptable salts in a known manner.

  一种制造抗生素7-(D-.alpha.-氨基-.alpha.-苯乙酰氨基)-3-甲基-3-头孢烯-4-羧酸(头孢氨苄)及其药学上可接受的盐的过程。该过程包括在双溶剂混合物中，在-20至-65℃的温度下，在吡啶衍生的双催化剂混合物的存在下，将D-(-)-α-苯基甘氨酸的恩酰保护钾盐(Dane盐)与酸氯化物反应。得到的混合酸酐与7-氨基去乙酰头孢菌素酸(7-ADCA)的烷基胍盐溶液在-10℃至-65℃的温度下缩合，然后用水矿酸水解产物的恩胺衍生物，同时在醇作为共溶剂的情况下沉淀抗生素。如果需要，可以以已知的方式将头孢氨苄转化为其药学上可接受的盐。
• Therapeutic human antipseudomonas aeruginosa antibodies
  申请人：Merck & Co., Inc.

  公开号：EP0256713A2

  公开（公告）日：1988-02-24

  Human lymphoblastoid cell lines and hybridomas are developed which secrete antibodies specifically reactive with lipopolysaccharide that is present on the surface of Pseudomonas aeruginosa. The individual monoclonal antibodies are immunospecific for one or more of the Fisher immunotypes of P. aeruginosa. The anti-Pseudomonas monoclonal anti­bodies are used individually or in combination to therapeutically or prophylactically treat P. aeruginosa infections. One or more of the monoclonal antibodies are co-administered with one or more antibiotics to therapeutically or prophylactically treat immunocompromised and immunosuppressed individuals.

  人类淋巴母细胞系和杂交瘤被开发出来，它们能分泌与铜绿假单胞菌表面的脂多糖特异性反应的抗体。单克隆抗体对铜绿假单胞菌的一种或多种费舍尔免疫型具有免疫特异性。抗铜绿假单胞菌单克隆抗体可单独或联合用于治疗或预防铜绿假单胞菌感染。一种或多种单克隆抗体可与一种或多种抗生素联合使用，用于治疗或预防免疫功能低下和免疫抑制个体。