盐酸匹美西林 | 32887-03-9

• 物质功能分类: 分析化学 - 标准品 - 药典标准品和杂质标准品
• 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
• 中文名称: 盐酸匹美西林
• 英文名称: pivmecillinam hydrochloride
• 英文别名: Selexid；2,2-dimethylpropanoyloxymethyl (2S,5R,6R)-6-(azepan-1-ylmethylideneamino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;hydron;chloride
• CAS: 32887-03-9
• 化学式: C₂₁H₃₃N₃O₅S*ClH
• 分子量: 476.037
• InChiKey: UHPXMYLONAGUPC-WKLLBTDKSA-N

物化性质

• 熔点：
  172-173°
• 比旋光度：
  D20 +219° (c = 1 in 0.1N HCl)
• 溶解度：
  易溶于水、无水乙醇和甲醇，微溶于丙酮。

计算性质

• 辛醇/水分配系数(LogP)：
  2.83
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.81
• 拓扑面积：
  114
• 氢给体数：
  1
• 氢受体数：
  7

ADMET

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用总结：氨苄青霉素（pivmecillinam；美西林戊酸酯）在美国没有商业销售，但在国际上市场有售。有限的信息表明，氨苄青霉素在乳汁中产生的水平较低，预计不会对哺乳婴儿造成不良影响。监测哺乳婴儿是否有腹泻和鹅口疮。 ◉ 对哺乳婴儿的影响：截至修订日期，未找到相关的已发布信息。 ◉ 对泌乳和母乳的影响：截至修订日期，未找到相关的已发布信息。

◉ Summary of Use during Lactation:Amdinocillin (pivmecillinam; the pivaloyl ester of mecillinam) is not commercially available in the United States, but is marketed internationally. Limited information indicates that amdinocillin produces low levels in milk that are not expected to cause adverse effects in breastfed infants. Monitor the breastfed infant for diarrhea and thrush. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.

来源:Drugs and Lactation Database (LactMed)

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335
• 储存条件：
  -20℃

制备方法与用途

生物活性方面，Pivmecillinam hydrochloride（FL-1039 hydrochloride）是 mecillinam 的口服前体药物，具有广谱抗菌作用。

文献信息

• METHODS AND COMPOSITIONS FOR TREATING INFECTION
  申请人：UNIVERSITY OF ROCHESTER

  公开号：US20150238473A1

  公开（公告）日：2015-08-27

  Provided herein are compositions and methods for treating or preventing infection.

  本文提供了用于治疗或预防感染的组合物和方法。
• 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。
• External preparation for skin diseases containing nitroimidazole
  申请人：——

  公开号：US20030092754A1

  公开（公告）日：2003-05-15

  An external preparation for skin disease which comprises a nitroimidazole derivative represented by the following formula (I): 1 wherein R 1 , R 3 and R 4 may be the same or different and represent a hydrogen atom, a nitro group, a lower alkyl group, a substituted lower alkyl group, a lower alkenyl group, or a substituted lower alkenyl group; and R 2 represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group and a lower alkenyl group or a substituted lower alkenyl group, provided that any one of R 1 , R 3 and R 4 is a nitro group.

  一种外用制剂，用于皮肤疾病，包括以下式(I)所代表的硝基咪唑衍生物：1其中R1、R3和R4可以相同也可以不同，并表示氢原子、硝基、低烷基、取代的低烷基、低烯基或取代的低烯基；R2表示氢原子、低烷基、取代的低烷基和低烯基或取代的低烯基，只要R1、R3和R4中的任何一个是硝基。
• POLYVINYL ALCOHOL PARTICLES, PHARMACEUTICAL BINDER USING SAME, PHARMACEUTICAL TABLET, SUSTAINED-RELEASE PHARMACEUTICAL TABLET, AND METHOD FOR PRODUCING POLYVINYL ALCOHOL PARTICLES
  申请人：THE NIPPON SYNTHETIC CHEMICAL INDUSTRY CO., LTD.

  公开号：US20170209377A1

  公开（公告）日：2017-07-27

  Provided herein is a polyvinyl alcohol fine particle suitable for a pharmaceutical binder for obtaining a pharmaceutical tablet of properties including good sustained release, high hardness, and excellent friability. The polyvinyl alcohol tine particle of the present invention contains 25 mol % or more of a gauche structure in polyvinyl alcohol molecules within a 0.8-nm region inside the particle from the particle surface.

  本发明提供了一种聚乙烯醇细颗粒，适用于制备具有良好持续释放性、高硬度和优异易碎性等特性的药物片剂的药物粘合剂。本发明的聚乙烯醇细颗粒在颗粒表面内0.8纳米范围内的聚乙烯醇分子中含有25摩尔％或更多的 gauche 结构。
• Sweetener compositions and uses thereof
  申请人：AJINOMOTO CO. INC

  公开号：US20040105928A1

  公开（公告）日：2004-06-03

  The present invention provides compositions containing one or more aspartyl dipeptide derivatives represented by formulas (1) and/or (2) mixed with another high intensity sweetner, such Aspartame, sugar, sugar alcohol, and oligosaccharide; food, beverages, and/or medicinal products containing these compositions, methods of using the compositions to impart sweetness in food, beverages, and/or medicinal products to impart sweetness or suppress a bitter taste; and methods of making the compositions and products.

  本发明提供了一种含有一个或多个由式(1)和/或式(2)表示的天冬氨酰二肽衍生物与另一种高强度甜味剂混合的组合物；含有这些组合物的食品、饮料和/或药品；使用这些组合物在食品、饮料和/或药品中赋予甜味或抑制苦味的方法；以及制备这些组合物和产品的方法。其中，另一种高强度甜味剂可以是阿斯巴甜、糖、糖醇和寡糖。