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aztreonam

中文名称
——
中文别名
——
英文名称
aztreonam
英文别名
(2S,3S)-3-[[(2E)-2-(2-amino-1,3-thiazol-3-ium-4-yl)-2-(2-carboxypropan-2-yloxyimino)acetyl]amino]-2-methyl-4-oxoazetidine-1-sulfonate
aztreonam化学式
CAS
——
化学式
C13H17N5O8S2
mdl
——
分子量
435.439
InChiKey
WZPBZJONDBGPKJ-IYZXUIDESA-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):
    0.3
  • 重原子数:
    28
  • 可旋转键数:
    7
  • 环数:
    2.0
  • sp3杂化的碳原子比例:
    0.46
  • 拓扑面积:
    238
  • 氢给体数:
    4
  • 氢受体数:
    12

ADMET

毒理性
  • 肝毒性
氨曲南具有与其他β-内酰胺类抗生素相似的全身毒性,但目前尚不清楚它是否会引起类似青霉素或头孢菌素类抗生素引起的肝损伤。在高剂量静脉注射氨曲南治疗期间(10%至38%),无症状血清转氨酶升高很常见。这些酶异常通常是轻至中度的、无症状的、自限性的,并且不需要停药。与其它比较的抗生素相比,氨曲南治疗期间酶升高的发生略为常见。归因于氨曲南的明显肝损伤和黄疸的病例极为罕见,因为尚未有单个病例报告。因此,关于损伤的潜伏期或模式的资料。有报告称,在开始使用氨曲南后3至5天内出现明显的转氨酶升高的情况,但这些病例没有黄疸,且在停药后迅速解决。
Aztreonam has systemic toxicities that are similar to those of other beta lactam antibiotics, but it is unclear whether it can cause hepatic injury similar to that of the penicillins or cephalosporins. Asymptomatic serum aminotransferase elevations are common during high dose, intravenous aztreonam therapy (10% to 38%). The enzyme abnormalities are usually mild-to-moderate, asymptomatic, self-limited and not requiring drug discontinuation. Enzyme elevations occur slightly more commonly during aztreonam therapy than with other comparative antibiotics. Cases of frank liver injury and jaundice attributable to aztreonam must be extremely rare as no individual cases have been reported. For this reason, there is no data regarding the latency or pattern of the injury. Instances of marked aminotransferase elevations within 3 to 5 days of starting aztreonam have been reported, but these cases were without jaundice and resolved rapidly once the drug was stopped.
来源:LiverTox
毒理性
  • 在妊娠和哺乳期间的影响
◉ 母乳喂养期间使用总结:有限的信息表明,阿兹特罗胺在乳汁中的水平较低,预计不会对哺乳婴儿造成不良影响。偶尔有报道指出,婴儿的胃肠道菌群受到干扰,导致腹泻或鹅口疮,但这些影响尚未得到充分评估。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,吸入妥布霉素与母乳喂养相容。阿兹特罗胺适用于哺乳期母亲。 ◉ 对哺乳婴儿的影响:截至修订日期,未找到相关已发布信息。 ◉ 对泌乳和母乳的影响:截至修订日期,未找到相关已发布信息。
◉ Summary of Use during Lactation:Limited information indicates that aztreonam produces low levels in milk that are not expected to cause adverse effects in breastfed infants. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with beta-lactams, but these effects have not been adequately evaluated. A task force respiratory experts from Europe, Australia and New Zealand found that inhaled tobramycin is compatible with breastfeeding. Aztreonam is acceptable in nursing mothers. ◉ 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)

上下游信息

  • 上游原料
    中文名称 英文名称 CAS号 化学式 分子量

反应信息

  • 作为产物:
    描述:
    氨曲南 作用下, 生成 aztreonam
    参考文献:
    名称:
    Stability of aztreonam in AZACTAM
    摘要:
    The influence of temperature and relative humidity on the stability of aztreonam in AZACTAM was investigated. Changes of the concentration of aztreonam were followed using the HPLC method with UV detection. The first-order rate constants of the reversible reaction of isomerization Z-aztreonam right harpoon over left harpoonE-aztreonam and the parallel reaction Z-aztreonam-->products were determined at RH=76.4% and T=313, 323, 333, 343 and 353 K, and at T=343 K and RH=50.9%, 60.5%, 66.5% and 76.4%. The thermodynamic parameters-energy, enthalpy and entropy of these reactions were calculated.
    DOI:
    10.1016/j.farmac.2005.04.009
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文献信息

  • Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
    申请人:Vertex Pharmaceuticals Incorporated
    公开号:US20150231142A1
    公开(公告)日:2015-08-20
    The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
    本发明涉及含有上皮钠通道活性抑制剂与至少一种ABC转运蛋白调节剂化合物(A式、B式、C式或D式)的药物组合物。该发明还涉及这些药物配方,以及使用这些组合物治疗CFTR介导的疾病,特别是囊性纤维化的方法。
  • Eflornithine Prodrugs, Conjugates and Salts, and Methods of Use Thereof
    申请人:Xu Feng
    公开号:US20100120727A1
    公开(公告)日:2010-05-13
    In one aspect, the present invention provides a composition of a covalent conjugate of an eflornithine analog with an anti-inflammatory drug. In another aspect, the present invention provides a composition of an eflornithine prodrug. In another aspect, the present invention provides a composition of an eflornithine or its derivatives aspirin salt. In another aspect, the present invention provides methods for treating or preventing cancer using the conjugates or salts of eflornithine analogs or eflornithine prodrugs.
    在一个方面,本发明提供了一种氟硝西汀类似物与抗炎药物的共价结合物的组合物。在另一个方面,本发明提供了一种氟硝西汀前药的组合物。在另一个方面,本发明提供了一种氟硝西汀或其衍生物水杨酸盐的组合物。在另一个方面,本发明提供了使用氟硝西汀类似物或氟硝西汀前药的共轭物或盐来治疗或预防癌症的方法。
  • [EN] 3,5-DIAMINO-6-CHLORO-N-(N-(4-PHENYLBUTYL)CARBAMIMIDOYL) PYRAZINE-2- CARBOXAMIDE COMPOUNDS<br/>[FR] COMPOSÉS 3,5-DIAMINO -6-CHLORO-N-(N- (4-PHÉNYLBUTYL)CARBAMIMIDOYL) PYRAZINE-2-CARBOXAMIDE
    申请人:PARION SCIENCES INC
    公开号:WO2014099673A1
    公开(公告)日:2014-06-26
    The present invention relates compounds of the formula: or pharmaceutically acceptable salts thereof, useful as sodium channel blockers, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including cystic fibrosis, chronic obstructive pulmonary disease, asthma, bronchiectasis, acute and chronic bronchitis, emphysema, and pneumonia.
    本发明涉及以下化合物的公式:或其药学上可接受的盐,用作钠通道阻滞剂,以及含有这些化合物的组合物,制备这些化合物的方法,以及在促进粘膜表面水合和治疗包括囊性纤维化、慢性阻塞性肺病、哮喘、支气管扩张、急性和慢性支气管炎、肺气肿和肺炎等疾病的治疗方法。
  • CHLORO-PYRAZINE CARBOXAMIDE DERIVATIVES WITH EPITHELIAL SODIUM CHANNEL BLOCKING ACTIVITY
    申请人:Parion Sciences, Inc.
    公开号:US20140171447A1
    公开(公告)日:2014-06-19
    This invention provides compounds of the formula I: and their pharmaceutically acceptable salts, useful as sodium channel blockers, compositions containing the same, therapeutic methods and uses for the same and processes for preparing the same.
    这项发明提供了式I的化合物及其药用盐,可用作钠通道阻滞剂,包含这些化合物的组合物,以及用于这些化合物的治疗方法和用途,以及制备这些化合物的方法。
  • [EN] DERIVATIVES OF AMANITA TOXINS AND THEIR CONJUGATION TO A CELL BINDING MOLECULE<br/>[FR] DÉRIVÉS DE TOXINES D'AMANITES ET LEUR CONJUGAISON À UNE MOLÉCULE DE LIAISON CELLULAIRE
    申请人:HANGZHOU DAC BIOTECH CO LTD
    公开号:WO2017046658A1
    公开(公告)日:2017-03-23
    Derivatives of Amernita toxins of Formula (I), wherein, formula (a) R 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9, R 10, X, L, m, n and Q are defined herein. The preparation of the derivatives. The therapeutic use of the derivatives in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.
    Amernita毒素的衍生物的化学式(I),其中,化学式(a)中的R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、X、L、m、n和Q在此处被定义。这些衍生物的制备。这些衍生物在靶向治疗癌症、自身免疫性疾病和传染病中的治疗用途。
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