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尼拉霉素 | 11048-13-8

中文名称
尼拉霉素
中文别名
——
英文名称
Tobramycin
英文别名
4,6-diamino-3-[(3-amino-3-deoxyhexopyranosyl)oxy]-2-hydroxycyclohexyl 2,6-diamino-2,3,6-trideoxy-;Nebramycin;4-amino-2-[4,6-diamino-3-[3-amino-6-(aminomethyl)-5-hydroxyoxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-6-(hydroxymethyl)oxane-3,5-diol
尼拉霉素化学式
CAS
11048-13-8
化学式
C18H37N5O9
mdl
MFCD00599594
分子量
467.52
InChiKey
NLVFBUXFDBBNBW-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

计算性质

  • 辛醇/水分配系数(LogP):
    -6.2
  • 重原子数:
    32
  • 可旋转键数:
    6
  • 环数:
    3.0
  • sp3杂化的碳原子比例:
    1.0
  • 拓扑面积:
    268
  • 氢给体数:
    10
  • 氢受体数:
    14

ADMET

毒理性
  • 在妊娠和哺乳期间的影响
◉ 母乳喂养期间使用概述:妥布霉素在母乳中的排泄量很少。新生儿显然会吸收少量其他氨基糖苷类药物,但在典型的每日三次剂量下,血清水平远低于治疗新生儿感染时达到的水平,因此妥布霉素的系统影响不太可能发生。年龄较大的婴儿吸收的妥布霉素会更少。由于在多次每日剂量方案中,母乳中妥布霉素水平的变异性很小,因此在与剂量相关的哺乳时机上减少婴儿暴露几乎没有或没有好处。对于单日剂量方案,尚无数据。监测婴儿可能出现的影响胃肠道菌群的情况,如腹泻、念珠菌病(例如,鹅口疮、尿布疹)或罕见的情况下,粪便中出现血液,提示可能存在抗生素相关性结肠炎。 母亲使用含有妥布霉素的耳滴或眼滴对哺乳婴儿几乎没有或没有风险。一个由欧洲、澳大利亚和新西兰的呼吸专家组成的小组发现,吸入妥布霉素与哺乳是相容的。 ◉ 对哺乳婴儿的影响:一名婴儿在产后第4个月之前一直母乳喂养(喂养程度未说明)。在2个月大时,他的母亲因囊性纤维化加重而接受了为期2周的妥布霉素150毫克,每日三次加美罗培南的治疗。在母亲治疗期间,婴儿的大便模式没有变化,在6个月大时肾功能正常。 ◉ 对泌乳和母乳的影响:截至修订日期,没有找到相关的已发布信息。
◉ Summary of Use during Lactation:Tobramycin is poorly excreted into breastmilk. Newborn infants apparently absorb small amounts of other aminoglycosides, but serum levels with typical three times per day dosages are far below those attained when treating newborn infections and systemic effects of tobramycin are unlikely. Older infants would be expected to absorb even less tobramycin. Because there is little variability in the milk tobramycin levels during multiple daily dose regimens, timing breastfeeding with respect to the dose is of little or no benefit in reducing infant exposure. Data are not available with single daily dose regimens. Monitor the infant for possible effects on the gastrointestinal flora, such as diarrhea, candidiasis (e.g., thrush, diaper rash) or rarely, blood in the stool indicating possible antibiotic-associated colitis. Maternal use of an ear drop or eye drop that contains tobramycin presents little or no risk for the nursing infant. A task force respiratory experts from Europe, Australia and New Zealand found that inhaled tobramycin is compatible with breastfeeding. ◉ Effects in Breastfed Infants:An infant was breastfed (extent not stated) until the 4th month postpartum. At 2 months of age, his mother was given a 2-week course of tobramycin 150 mg three times daily plus meropenem for a cystic fibrosis exacerbation. infant displayed no change in stool pattern during the maternal treatment and had normal renal function at 6 months of age. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.
来源:Drugs and Lactation Database (LactMed)

反应信息

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文献信息

  • Active agent delivery systems and methods for protecting and administering active agents
    申请人:Mickle Travis
    公开号:US20070232529A1
    公开(公告)日:2007-10-04
    The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.
    本发明涉及活性物质输送系统,更具体地涉及包含氨基酸(作为单个氨基酸或肽)与活性物质共价连接的组合物以及用于给予共轭活性物质组合物的方法。
  • ACTIVE AGENT DELIVERY SYSTEMS AND METHODS FOR PROTECTING AND ADMINISTERING ACTIVE AGENTS
    申请人:Mickle Travis
    公开号:US20090253792A1
    公开(公告)日:2009-10-08
    The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.
    本发明涉及活性剂递送系统,更具体地涉及包含氨基酸(作为单个氨基酸或肽)与活性剂共价连接的组合物以及给予共轭活性剂组合物的方法。
  • ACTIVE AGENT DELIVERY SYSTEMS AND METHODS FOR PROTECTING AND ADMINISTERING ACTIVE AGENTS
    申请人:Mickle Travis
    公开号:US20090306228A1
    公开(公告)日:2009-12-10
    The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.
    本发明涉及活性剂递送系统,更具体地涉及包含氨基酸,作为单个氨基酸或肽,与活性剂共价结合的组合物以及用于给予共轭活性剂组合物的方法。
  • AMINOGLYCOSIDE DERIVATIVES AND NANO-ASSEMBLIES THEREOF, INCLUDING THOSE WITH QUORUM SENSING INHIBITORY FUNCTION
    申请人:Helmholtz-Zentrum für Infektionsforschung GmbH
    公开号:EP3421050A1
    公开(公告)日:2019-01-02
    The present invention relates to conjugates of aminoglycosides and terpenoids, in particular sesquiterpenoids. Furthermore, the present invention relates to nano-assemblies formed by the inventive conjugates and to a method for producing the conjugates and/or the nano-assemblies. The present invention also relates to the inventive conjugates and nano-assemblies for use in therapy, in particular for use in the treatment of infectious diseases. Particularly preferred embodiments of the present invention relate to farnesylated aminoglycosides and nano-assemblies thereof, in which farnesol and its derivatives do not only function as carrier for the aminoglycosides but do themselves have pharmaceutical activity upon cleavage of the conjugate, in particular quorum sensing inhibitory activity.
    本发明涉及氨基糖苷类和萜类,特别是倍半萜类的共轭物。此外,本发明还涉及由本发明共轭物形成的纳米组合物,以及生产共轭物和/或纳米组合物的方法。本发明还涉及用于治疗的本发明共轭物和纳米组合物,特别是用于治疗传染性疾病的共轭物和纳米组合物。本发明特别优选的实施方案涉及法呢醇化氨基糖苷类化合物及其纳米组合物,其中法呢醇及其衍生物不仅作为氨基糖苷类化合物的载体,而且在共轭物裂解后本身也具有药物活性,特别是定量感应抑制活性。
  • Compounds for treating biofilm infection
    申请人:Board of Regents, The University of Texas System
    公开号:US10272158B2
    公开(公告)日:2019-04-30
    In some aspects, pegylated aminoglycoside compounds are provided. In some embodiments, m-PEG-tobramycin compounds may be used to treat a biofilm infection or reduce or treat established biofilms. The present invention provides, in various aspects, compounds and methods for the treatment of infections, such as biofilm infections or chronic biofilm infections. The chronic biofilm infection may occur in wounds, implanted devices, immunocompromised patients, people with cystic fibrosis, eye infections, etc.
    在某些方面,提供了聚乙二醇化氨基糖苷化合物。在一些实施方案中,m-PEG-托布霉素化合物可用于治疗生物膜感染或减少或治疗已形成的生物膜。本发明在各个方面提供了治疗感染的化合物和方法,如生物膜感染或慢性生物膜感染。慢性生物膜感染可能发生在伤口、植入设备、免疫力低下的患者、囊性纤维化患者、眼部感染等。
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