amoxicillin sodium | 53512-15-5

• 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: amoxicillin sodium
• 英文别名: sodium amoxycillin；sodium amoxicillin；sodium;(2S,5R,6R)-6-[[2-amino-2-(4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate；sodium;4-[1-amino-2-[[(2S,5R,6R)-2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptan-6-yl]amino]-2-oxoethyl]phenolate
• CAS: 53512-15-5
• 化学式: C₁₆H₁₈N₃O₅S*Na
• 分子量: 387.392
• InChiKey: BYHDFCISJXIVBV-GJUCOGTPSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  -4.31
• 重原子数：
  26
• 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：
  161
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  amoxicillin 生成 amoxicillin sodium
  参考文献：
  名称：

  PEREZ-ARANDA, ORTEGA AUGUSTIN;RUZAFA, SANTIAGO C.;SERRA, FERNANDO R.

  摘要：

  DOI：

文献信息

• [EN] BETA-LACTAMASE INHIBITOR PRODRUG<br/>[FR] PROMEDICAMENT INHIBITEUR DE LA BETA-LACTAMASE
  申请人：PFIZER PROD INC

  公开号：WO2004108733A1

  公开（公告）日：2004-12-16

  Prodrugs of 6-β-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, each X is methylene, and Y is 0, or wherein R is H, each X is 0 and Y is methylene, and solvates thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention, or a solvate thereof, an optional beta-lactam antibiotic and at least one pharmaceutically acceptable carrier. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in 20 a mammal by administering an effective amount of a beta­lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.

  6-β-羟甲基青霉烷酸磺酸的前药具有以下结构，其中R为H或甲基，每个X为亚甲基，Y为0，或其中R为H，每个X为0，Y为亚甲基，以及其溶剂化合物。还披露了包括本发明的前药或其溶剂化合物、可选的β-内酰胺类抗生素和至少一种药用可接受载体的药物组合物。进一步披露了通过给哺乳动物投予有效量的β-内酰胺类抗生素和本发明的前药或其溶剂化合物的增效量来增加β-内酰胺类抗生素的治疗效果的方法。此外，还披露了通过给需要的哺乳动物投予本发明的药物组合物的治疗有效量来治疗哺乳动物的细菌感染的方法。
• [EN] BETA-LACTAMASE INHIBITOR PRODRUG<br/>[FR] PROMEDICAMENT INHIBITEUR DE BETA-LACTAMASE
  申请人：PFIZER PROD INC

  公开号：WO2004018484A1

  公开（公告）日：2004-03-04

  Prodrugs of 6-ß-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention, or a solvate thereof, an optional beta-lactam antibiotic and at least one pharmaceutically acceptable carrier. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a betalactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.

  6-ß-羟甲基青霉烷酸磺酸酯的前药具有结构，其中R为H或甲基，并公开其溶剂合物。还公开了包括本发明的前药或其溶剂合物、可选的β-内酰胺类抗生素和至少一种药用载体的药物组合物。进一步公开了通过给哺乳动物投予β-内酰胺类抗生素的有效量和本发明的前药或其溶剂合物的增效量来增加β-内酰胺类抗生素的治疗效果的方法。此外，还公开了通过给需要的哺乳动物投予本发明的药物组合物的治疗有效量来治疗哺乳动物的细菌感染的方法。
• GAMMA-AAPEPTIDES WITH POTENT AND BROAD-SPECTRUM ANTIMICROBIAL ACTIVITY
  申请人：Cai Jianfeng

  公开号：US20150274782A1

  公开（公告）日：2015-10-01

  The present invention is directed to a novel class of antimicrobial agents called γ-AApeptides. The current invention provides various categories of γ-AApeptides, for example, linear γ-AApeptides, cyclic γ-AApeptides, and lipidated γ-AApeptides. γ-AApeptides of the current invention are designed to exert antimicrobial activity while being stable and non-toxic. γ-AApeptides also do not appear to lead to the development of microbial resistance in treated microorganisms. Thus, the disclosed γ-AApeptides can be used for the treatment of various medical conditions associated with pathogenic microorganisms.

  本发明涉及一种新型类别的抗微生物药物，称为γ-AA肽。当前发明提供了各种类别的γ-AA肽，例如线性γ-AA肽、环状γ-AA肽和脂质化γ-AA肽。本发明的γ-AA肽被设计为具有抗微生物活性，同时稳定且无毒。γ-AA肽似乎也不会导致被治疗微生物体内微生物产生抗药性。因此，所披露的γ-AA肽可用于治疗与病原微生物相关的各种医疗状况。
• [EN] IMPROVED PROCESS FOR PREPARING AMOXICILLIN SODIUM<br/>[FR] PROCÉDÉ AMÉLIORÉ POUR PRÉPARER DU SODIUM D'AMOXICILLINE
  申请人：VARDHMAN CHEMTECH LTD

  公开号：WO2011158133A1

  公开（公告）日：2011-12-22

  An improved process for preparing sterile amoxicillin and an alkali metal salt thereof, wherein the said process involves the steps of: i) dissolving amoxicillin trihydrate in methyl acetate, methanol and triethylamine; ii) Passing the resulting solution through a series of filters iii) addition of mixture of sodium-2-ethylhexanoate, methyl acetate and methanol followed by addition of methyl acetate iv) crystallizing the product to obtain sterile amoxicillin sodium.

  一种改进的制备无菌阿莫西林及其碱金属盐的方法，其中所述方法包括以下步骤：i) 在甲酸甲酯、甲醇和三乙胺中溶解阿莫西林三水合物；ii) 将所得溶液通过一系列过滤器；iii) 加入2-乙基己酸钠、甲酸甲酯和甲醇的混合物，然后加入甲酸甲酯；iv) 结晶产物以获得无菌阿莫西林钠。
• Beta-lactamase inhibitor prodrug
  申请人：Marfat Anthony

  公开号：US20050004093A1

  公开（公告）日：2005-01-06

  Prodrugs of 6-β-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, each X is methylene, and Y is O, or wherein R is H, each X is O and Y is methylene, and solvates thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention, or a solvate thereof, an optional beta-lactam antibiotic and at least one pharmaceutically acceptable carrier. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a beta-lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.

  本发明揭示了6-β-羟甲基青霉烷酸磺酸酯的前药物，其结构为：其中R为氢或甲基，每个X为亚甲基，Y为氧，或其中R为氢，每个X为氧，Y为亚甲基，以及其溶剂化物。还揭示了包含本发明的前药物或其溶剂化物、可选的β-内酰胺类抗生素和至少一种药学上可接受的载体的制药组合物。此外，还揭示了通过给哺乳动物注射有效量的β-内酰胺类抗生素和本发明的前药物或其溶剂化物的增效剂量来提高β-内酰胺类抗生素的治疗效果的方法。此外，还揭示了通过给需要治疗细菌感染的哺乳动物注射本发明的制药组合物的治疗有效量来治疗细菌感染的方法。