2-[(1R,3S)-8-[(1R,3S)-3-(carboxymethyl)-5,10-dihydroxy-1-methyl-6,9-dioxo-3,4-dihydro-1H-benzo[g]isochromen-8-yl]-5,10-dihydroxy-1-methyl-6,9-dioxo-3,4-dihydro-1H-benzo[g]isochromen-3-yl]acetic acid

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 异色满醌
• 英文名称: 2-[(1R,3S)-8-[(1R,3S)-3-(carboxymethyl)-5,10-dihydroxy-1-methyl-6,9-dioxo-3,4-dihydro-1H-benzo[g]isochromen-8-yl]-5,10-dihydroxy-1-methyl-6,9-dioxo-3,4-dihydro-1H-benzo[g]isochromen-3-yl]acetic acid
• 化学式: C₃₂H₂₆O₁₄
• 分子量: 634.5
• InChiKey: FXTIILIJTTYSLT-WYUUTHIRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  46
• 可旋转键数：
  5
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  242
• 氢给体数：
  6
• 氢受体数：
  14

文献信息

• Amido macrolides
  申请人：Kosan Biosciences, Inc.

  公开号：US20030199458A1

  公开（公告）日：2003-10-23

  Various macrolide compounds such as those having the following formulas are provided where the variables have the values provided herein. 1

  各种大环内酯化合物，例如具有以下化学式的化合物，其中变量具有此处提供的值。
• Compositions for controlled delivery of pharmaceutically active compounds
  申请人：Murthy V.S.N. Yerramilli

  公开号：US20060093632A1

  公开（公告）日：2006-05-04

  The invention relates to pharmaceutical compositions that provide sustained-release of a pharmaceutically active compound and to methods of treating or preventing a condition in an animal by administering the pharmaceutical compositions to the animal by injection. When the pharmaceutical compositions are administered to an animal by injection, they form a drug depot that releases the pharmaceutically active compound over time. The pharmaceutical compositions can also be administered orally.

  该发明涉及提供药物组合物，该药物组合物提供药效活性化合物的持续释放，并且通过注射将药物组合物给动物以治疗或预防动物的某种疾病的方法。当将药物组合物通过注射给动物时，它们形成一个药物库，随着时间释放药效活性化合物。这些药物组合物也可以通过口服给予。
• Novel erythromycin derivatives
  申请人：Pfizer Inc.

  公开号：US20040067897A1

  公开（公告）日：2004-04-08

  The invention relates to novel erythromycin derivatives, particularly ones with novel C-13 R 13 substitutents, and to pharmaceutically acceptable salts thereof. The compounds of this invention are useful as antibacterial agents and antiprotozoa agents and for other applications (e.g., anticancer, atherosclerosis, gastric motility reduction, etc.) in mammals, including man, as well as in fish and. The invention also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial protozoa infections by administering such compounds. The invention also relates to methods of preparing such compounds and to intermediates useful in such preparation.

  该发明涉及新型红霉素衍生物，特别是具有新型C-13 R13取代基的红霉素衍生物，以及其药用盐。本发明的化合物可用作抗菌剂和抗原虫剂以及在哺乳动物（如人类）、鱼类等中的其他应用（例如，抗癌、动脉粥样硬化、胃动力减弱等）。该发明还涉及含有这种化合物的药物组合物，以及通过给予这种化合物来治疗细菌原虫感染的方法。该发明还涉及制备这种化合物的方法以及在制备中有用的中间体。
• Compositions and methods for activation and overexpression of secondary metabolites in microorganisms
  申请人：Prospective Research, Inc.

  公开号：US20180346871A1

  公开（公告）日：2018-12-06

  Methods and compositions herein provide non-naturally occurring γ-butyrolactones (GBLs) in racemic mixtures that increase efficiency and effectiveness of screening for production of antibiotics, and enhance yields and express silent pathways. Non-naturally occurring GBLs were synthesized and found to stimulate antibiotic production in several different streptomycete strains. Antibiotic production by Streptomyces coelicolor was induced by a racemic mixture of non-cognate stereoisomers of VB-D, seven of which are non-naturally occurring. Further, novel A-factor-type GBL analogs stimulated antibiotic production in S. coelicolor . Synthesis in response to the treatment with the non-cognates GBL was observed for known compounds including undecylprodigiosin, desferrioxamine and streptorubin B, as was synthesis of a compound of unknown structure. A group of 37 additional microbial strains was screened by principal component analysis to determine optimal concentrations of each of a panel of four non-cognate synthetic GBLs for addition to cultures with optimal stimulation of secondary metabolites, and large scale fermentations were analyzed and product enhancement by the GBLs was observed.

  本文提供的方法和组合物提供了非自然存在的γ-丁内酯（GBLs）的混合物，可增加筛选生产抗生素的效率和有效性，并增强产量和表达沉默途径。已合成非自然存在的GBLs，并发现它们能刺激几种不同链霉菌菌株的抗生素产生。通过非同源立体异构体VB-D的混合物（其中七种非自然存在）可以诱导链霉菌共色素的抗生素产生。此外，新型A因子型GBL类似物刺激了S. coelicolor的抗生素产生。已知化合物，包括十一烷基紫质素，去铁蛋白和链霉红素B，以及一种未知结构的化合物，对非同源GBL的处理作出了合成反应。通过主成分分析筛选了37个额外的微生物菌株，以确定每种四种非同源合成GBL的最佳浓度，以优化次生代谢物的刺激，并对大规模发酵进行了分析，观察到GBLs的产物增强效果。
• [EN] FK506 AND FK520 ANALOGUES AND THEIR PHARMACEUTICAL USES<br/>[FR] ANALOGUES DE FK506 ET PK520 ET LEURS UTILISATIONS PHARMACEUTIQUES
  申请人：BIOTICA TECH LTD

  公开号：WO2010106366A1

  公开（公告）日：2010-09-23

  The present invention relates to novel FK506 and FK520 analogues and strains generated by replacing the natural loading module of the FK506 or FK520 polyketide synthase (PKS) with the avermectin or an avermectin-like PKS loading module and optionally feeding non-natural starter units to these strains and to use of such compounds in therapy.

  本发明涉及新颖的FK506和FK520类似物以及通过使用avermectin或类似于avermectin的多酮合成酶（PKS）的装载模块替换FK506或FK520 PKS的自然装载模块并可选择性地向这些菌株提供非自然起始单元而生成的菌株，以及这些化合物在治疗中的应用。