carbonic acid 2,5-dioxo-pyrrolidin-1-yl ester propyl ester | 112884-31-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: carbonic acid 2,5-dioxo-pyrrolidin-1-yl ester propyl ester
• 英文别名: (2,5-Dioxopyrrolidin-1-yl) propyl carbonate
• CAS: 112884-31-8
• 化学式: C₈H₁₁NO₅
• 分子量: 201.179
• InChiKey: RNRROHBUPRKLLQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  72.9
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-amino-6-(butylthio)-2-cyclohexyl-1H-benzo[d]imidazole 、 carbonic acid 2,5-dioxo-pyrrolidin-1-yl ester propyl ester 以 二氯甲烷 为溶剂， 反应 16.0h， 以62%的产率得到6-(butylthio)-2-cyclohexyl-5-propoxycarbonylamino-1H-benzo[d]imidazole
  参考文献：
  名称：

  Design, synthesis and evaluation of novel 2,5,6-trisubstituted benzimidazoles targeting FtsZ as antitubercular agents

  摘要：

  Filamenting temperature-sensitive protein Z (FtsZ), an essential cell division protein, is a promising target for the drug discovery of new-generation antibacterial agents against various bacterial pathogens. As a part of SAR studies on benzimidazoles, we have synthesized a library of 376 novel 2,5,6-trisubstituted benzimidazoles, bearing ether or thioether linkage at the 6-position. In a preliminary HTP screening against Mtb H37Rv, 108 compounds were identified as hits at a cut off concentration of 5 mu g/mL. Among those hits, 10 compounds exhibited MIC values in the range of 0.63-12.5 mu g/mL. Light scattering assay and TEM analysis with the most potent compound 5a clearly indicate that its molecular target is Mtb-FtsZ. Also, the K-d of 5a with Mtb-FtsZ was determined to be 1.32 mu M. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2014.03.035

文献信息

• [EN] GLUCOSE-SENSITIVE PEPTIDE HORMONES<br/>[FR] HORMONES PEPTIDIQUES SENSIBLES AU GLUCOSE
  申请人：GUBRA APS

  公开号：WO2018115462A1

  公开（公告）日：2018-06-28

  The present invention relates to a conjugate of the formula P-L-I, wherein P is a peptide hormone effecting the metabolism of carbohydrates in vivo, L is a hydrolysable linker molecule consisting of Lp and Li, and I is a molecule capable of inhibiting the effect of the peptide hormone P on the metabolism of carbohydrates in vivo. Under in vivo conditions, the conjugate is the major compound. When the concentration of glucose increases in vivo, the concentration of the peptide hormone effecting the metabolism of carbohydrates in vivo also increases.

  本发明涉及一种公式为P-L-I的结合物，其中P是一种肽激素，在体内影响碳水化合物代谢，L是由Lp和Li组成的可水解连接分子，I是一种能够抑制肽激素P对体内碳水化合物代谢影响的分子。在体内条件下，该结合物是主要化合物。当体内葡萄糖浓度增加时，影响碳水化合物代谢的肽激素浓度也会增加。
• [EN] POLYMER OR POLYCONDENSATE BASED ON PEPTIDE, LINKER AND OPTIONALLY OTHER MONOMERS AND METHOD FOR PREPARING THE SAME<br/>[FR] POLYMÈRE OU POLYCONDENSAT À BASE DE PEPTIDE, DE COUPLEUR ET ÉVENTUELLEMENT D'AUTRES MONOMÈRES ET SON PROCÉDÉ DE PRÉPARATION
  申请人：ECOLE POLYTECHNIQUE FED LAUSANNE EPFL

  公开号：WO2021053198A1

  公开（公告）日：2021-03-25

  The present invention concerns a method for producing polymers suitable as carrier-free delivery system of bioactive molecules, in particular bioactive peptides. The method comprises the polycondensation of one or more different monomers, including monomers comprising the peptides, monomers comprising a cross-linker and, optionally, monomers comprising an adjuvant. The invention also relates to the polymers obtained by the method, which are suitable as medicaments, such as vaccines. In a particular embodiment, the bioactive peptide is a neoantigen and the polymer is used as a cancer vaccine.

  本发明涉及一种用于生产适用作无载体生物活性分子传递系统的聚合物的方法，特别是生物活性肽。该方法包括聚合一种或多种不同的单体，包括包含肽的单体、包含交联剂的单体，以及可选地包含辅助剂的单体。该发明还涉及通过该方法获得的聚合物，适用作药物，如疫苗。在一个特定实施例中，生物活性肽是新抗原，聚合物被用作癌症疫苗。
• CRYSTALLINE FORMS OF AN ANTIVIRAL COMPOUND
  申请人：Gilead Sciences, Inc.

  公开号：US20170267694A1

  公开（公告）日：2017-09-21

  Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.

  抗HCV化合物的晶体形式(1aR,5S,8S,9S,10R,22aR)-5-叔丁基-N-[(1R,2R)-2-(二氟甲基)-1-[(1-甲基环丙基)磺酰]氨基}环丙基]-9-乙基-18,18-二氟-14-甲氧基-3,6-二氧-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-十四环-8H-7,10-甲烷基环丙[18,19][1,10,3,6]二氧二氮杂环十九烷醯胺(化合物I)已在固态下制备和表征。此外，还提供了制造过程和使用晶体形式的方法。
• BIOCOMPATIBLE CROSSLINKED HYDROGELS, DRUG-LOADED HYDROGELS AND METHODS OF USING THE SAME
  申请人：He Yuehua

  公开号：US20090324720A1

  公开（公告）日：2009-12-31

  Disclosed are hydrogel compositions formed by the mixture of a tetramethylmethane substituted with one or more polyethylene glycols, and wherein each polyethylene glycol substituent is independently further substituted with one or more electrophilic groups, and a tetramethylmethane substituted with one or more polyethylene glycols, and wherein each polyethylene glycol substituent is independently further substituted with one or more nucleophilic groups. Disclosed are also methods of preparing the above hydrogels. The hydrogel compositions can further comprise pharmaceuticals, such as analgesics or local anesthetics. Disclosed are also methods of sealing a wound, preventing post-surgical adhesion, and reducing post-surgical pain using the disclosed hydrogels.

  本发明揭示了一种由四甲基甲烷与一种或多种聚乙二醇混合而成的水凝胶组合物，其中每个聚乙二醇取代基独立地进一步取代有一种或多种亲电基团，以及由一种或多种聚乙二醇取代基独立地进一步取代有一种或多种亲核基团的四甲基甲烷与一种或多种聚乙二醇混合而成的水凝胶组合物。本发明还揭示了制备上述水凝胶的方法。水凝胶组合物还可以包含药物，例如止痛药或局部麻醉剂。本发明还揭示了使用上述水凝胶密封伤口、预防术后粘连和减轻术后疼痛的方法。
• METHODS TO INCREASE THE PHOTOSTABILITY OF DYES
  申请人：Hahn Klaus

  公开号：US20110046000A1

  公开（公告）日：2011-02-24

  The presently disclosed subject matter provides dyes having an improved photostability, biosensors comprising such dyes, and methods of use thereof, including methods for detecting target molecules in a sample under test and for live-cell imaging. The dyes can include a binding member, including a biomolecule or fragments thereof, which can interact with target molecules of interest and can be specific to a given conformational state or covalent modification, e.g., phosphorylation, of the target molecule. The presently disclosed dyes can be used for detecting changes in the binding, conformational change, or posttranslational modification of the target molecule.

  所述主题提供了具有改善光稳定性的染料、包括此类染料的生物传感器以及其使用方法，包括用于检测样品中的靶分子和用于活细胞成像的方法。该染料可以包括结合成员，包括生物分子或其片段，其可以与感兴趣的靶分子相互作用，并且可以特定于给定的构象状态或靶分子的共价修饰，例如磷酸化。目前披露的染料可用于检测靶分子的结合、构象变化或后翻译修饰的变化。