O''-Stearoyl-erythromycin | 97327-17-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: O''-Stearoyl-erythromycin
• 英文别名: [(2S,3R,4S,6R)-4-(dimethylamino)-2-[[(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-2,10-dioxo-oxacyclotetradec-6-yl]oxy]-6-methyloxan-3-yl] octadecanoate
• CAS: 97327-17-8
• 化学式: C₅₅H₁₀₁NO₁₄
• 分子量: 1000.41
• InChiKey: ICHUVKHKIVZNJJ-HXFLLBKSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  11.7
• 重原子数：
  70
• 可旋转键数：
  25
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.95
• 拓扑面积：
  200
• 氢给体数：
  4
• 氢受体数：
  15

反应信息

• 作为产物：
  描述：

  十八烷酰氯 、 红霉素 在 碳酸氢钠 、 丙酮 作用下， 生成 O''-Stearoyl-erythromycin
  参考文献：
  名称：

  Clark; Varner, Antibiotics and Chemotherapy, 1957, vol. 7, p. 487

  摘要：

  DOI：

文献信息

• [EN] PEPTIDE-BASED MULTIPLE-DRUG DELIVERY VEHICLE<br/>[FR] VÉHICULE D'ADMINISTRATION DE MÉDICAMENTS MULTIPLES À BASE DE PEPTIDES
  申请人：ARIEL-UNIVERSITY RES AND DEV COMPANY LTD

  公开号：WO2017068577A1

  公开（公告）日：2017-04-27

  A molecular structure comprising a targeting moiety, a multi-functional peptide platform and a plurality of controllably released bioactive agents attached thereto is provided herein.

  本文提供了一种包括靶向基团、多功能肽平台和附着在其上的多种可控释放的生物活性剂的分子结构。
• [EN] ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS<br/>[FR] ANTI-INFECTIEUX A BASE D'ISOTHIAZOLOQUINOLONES ET DE SELS CORRESPONDANTS
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2005019228A1

  公开（公告）日：2005-03-03

  The invention provides compounds and salts of Formula (I) and Formula (II): which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of a compound of Formula (I) or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

  本发明提供了具有抗菌活性的公式(I)和公式(II)的化合物及盐类：本发明还提供了用于制造公式(I)和公式(II)化合物的新的合成中间体。变量A1、R2、R3、R5、R6、R7、A8和R9在此文中定义。本文披露的某些公式(I)和公式(II)化合物是细菌DNA合成和细菌复制的强效和选择性抑制剂。本发明还提供了含有一种或多种公式(I)或公式(II)化合物以及一种或多种载体、辅料或稀释剂的抗菌组合物，包括药物组合物。这样的组合物可以只含有公式(I)或公式(II)的化合物作为唯一的活性成分，也可以含有公式(I)或公式(II)的化合物与一种或多种其他活性成分的组合。本发明还提供了用于治疗动物微生物感染的方法。
• Compositions and Methods for Preventing or Treating Diseases, Conditions, or Processes Characterized by Aberrant Fibroblast Proliferation and Extracellular Matrix Deposition
  申请人：MOERAE MATRIX, INC.

  公开号：US20160136234A1

  公开（公告）日：2016-05-19

  The described invention provides compositions and methods for reducing progression of a fibrosis in a tissue of a subject selected from liver, kidney or vascular fibrosis, the progression of the fibrosis being characterized by aberrant fibroblast proliferation and extracellular matrix deposition in the tissue. The method includes administering a therapeutic amount of a pharmaceutical composition containing a polypeptide having the amino acid sequence YARAAARQARAKALARQLGVAA (SEQ ID NO: 1) or functional equivalent thereof, and a pharmaceutically acceptable carrier, wherein the therapeutic amount of the polypeptide is effective to reduce progression of the fibrosis, to treat remodeling of the tissue, or a combination thereof.

  描述的发明提供了一种用于减少主体选定组织中的纤维化进展的组成和方法，该选定组织来自肝纤维化、肾纤维化或血管纤维化，纤维化的进展在组织中以异常成纤维细胞增殖和细胞外基质沉积为特征。该方法包括施用含有具有氨基酸序列YARAAARQARAKALARQLGVAA（SEQ ID NO: 1）或其功能等效物的多肽的药物治疗量，以及药学上可接受的载体，其中多肽的治疗量有效于减少纤维化的进展，治疗组织的重塑，或其组合。
• GLUTATHIONE-CHOLESTEROL DERIVATIVES AS BRAIN TARGETING AGENTS
  申请人：South Dakota Board of Regents

  公开号：US20200048305A1

  公开（公告）日：2020-02-13

  The present invention describes compositions containing cholesterol-linker-glutathione conjugates for targeting the brain by overcoming barrier entry to the CNS through the blood brain barrier (BBB), including micelle and liposome forms of such compositions. In addition, methods for treating subjects by administering such compositions are also disclosed.

  本发明描述了含有胆固醇-连接剂-谷胱甘肽共轭物的组合物，通过克服血脑屏障（BBB）进入中枢神经系统的屏障入口，包括这些组合物的胶束和脂质体形式。此外，还公开了通过给予这些组合物治疗受试者的方法。
• [EN] THERANOSTIC CONJUGATES<br/>[FR] CONJUGUÉS THÉRANOSTIQUES
  申请人：ARIEL SCIENT INNOVATIONS LTD

  公开号：WO2021009759A1

  公开（公告）日：2021-01-21

  Provided herein is a drug delivery (DD) system for ratiometric luminescence determination of drug release degree in drug delivery monitoring, which includes a drug, a switchable reporter and non-switchable reporter providing two distinguishable signals for detection; or a single switchable reporter providing two distinguishable signals for detection, and a cleavable linker connecting a drug to a switchable reporter, as well as a method for ratiometric luminescence determination of drug release in a target in vivo or in vitro), which is effected by administering the DD system provided herein that is capable of releasing a drug from the DD system, measuring two luminescent signals provided by the switchable reporter and the non-switchable reporter, or the single switchable reporter, determining the ratio between these two luminescence signals, and determining the drug release degree through the ratio between the two luminescence signals.

  本文提供了一种药物递送（DD）系统，用于药物递送监测中药物释放程度的比例荧光测定，该系统包括一种药物、一种可切换的报告物和一种不可切换的报告物，用于提供两种可区分的信号以进行检测；或者一种单一可切换的报告物，用于提供两种可区分的信号以进行检测，以及一种可切割的连接剂，连接药物和可切换的报告物，以及一种比例荧光测定方法，用于在目标（体内或体外）中测定药物释放，通过给予本文提供的能够从DD系统中释放药物的DD系统，测量可切换的报告物和不可切换的报告物提供的两个发光信号，或者单一可切换的报告物，确定这两个发光信号之间的比例，并通过这两个发光信号之间的比例确定药物释放程度。