5-(1,2-dithiolan-3-yl)-N-(2-hydroxyethyl)pentanamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二硫杂环戊烷
• 英文名称: 5-(1,2-dithiolan-3-yl)-N-(2-hydroxyethyl)pentanamide
• 英文别名: 5-(dithiolan-3-yl)-N-(2-hydroxyethyl)pentanamide
• 化学式: C₁₀H₁₉NO₂S₂
• 分子量: 249.398
• InChiKey: UKKQRPFDGXMFAQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  15
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  99.9
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-(1,2-dithiolan-3-yl)-N-(2-hydroxyethyl)pentanamide 以75 %的产率得到N-[2-[2-cyanoethoxy-[di(propan-2-yl)amino]phosphanyl]oxyethyl]-5-(dithiolan-3-yl)pentanamide
  参考文献：
  名称：

  Genetic probe for the detection of a single nucleotide polymorphism (SNP) or a single nucleotide modification of a target nucleic acid

  摘要：

  The present invention relates to a genetic probe comprising: a nanoparticle; an oligonucleotide probe anchored to the surface of the nanoparticle, comprising an oligonucleotide backbone with a tag incorporated therein via a linker group; and a reference probe anchored to the surface of the nanoparticle, wherein the reference probe comprises a marker; wherein either (a) the tag is an organic fluorescent tag and the marker is a transition metal-based fluorescent marker; or (b) the tag is a redox-active tag and the marker is a transition metal-based redox-active marker. The invention also relates to a composition or kit containing a probe of the invention.

  公开号：

  US12043865B2
• 作为产物：
  描述：

  C.I.酸性橙108 、 R-(+)-硫辛酸 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N-乙基吗啉 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以73 %的产率得到5-(1,2-dithiolan-3-yl)-N-(2-hydroxyethyl)pentanamide
  参考文献：
  名称：

  Genetic probe for the detection of a single nucleotide polymorphism (SNP) or a single nucleotide modification of a target nucleic acid

  摘要：

  The present invention relates to a genetic probe comprising: a nanoparticle; an oligonucleotide probe anchored to the surface of the nanoparticle, comprising an oligonucleotide backbone with a tag incorporated therein via a linker group; and a reference probe anchored to the surface of the nanoparticle, wherein the reference probe comprises a marker; wherein either (a) the tag is an organic fluorescent tag and the marker is a transition metal-based fluorescent marker; or (b) the tag is a redox-active tag and the marker is a transition metal-based redox-active marker. The invention also relates to a composition or kit containing a probe of the invention.

  公开号：

  US12043865B2

文献信息

• Dithiolan derivatives, their preparation and their therapeutic effect
  申请人：Sankyo Company, Limited

  公开号：US06013663A1

  公开（公告）日：2000-01-11

  A compound of formula (I): ##STR1## wherein one of m and n represents 0, and the other represents 0, 1 or 2; k represents 0 or 1 to 12; R.sup.1 is hydrogen, an aryl, a heterocyclic, an alkyl, a hydroxy or --OR.sup.7, wherein R.sup.7 is an alkyl, an alkenyl or an aralkyl; A is --CON(R.sup.2)SO.sub.2--, wherein R.sup.2 is hydrogen, an alkyl or an aralkyl; B is a single bond; and pharmaceutically acceptable salts thereof. The compounds have the ability to enhance the activity of glutathione reductase and can therefore be used for the treatment and prevention of a variety of diseases including cataracts.

  式（I）的化合物：其中m和n中的一个表示0，另一个表示0、1或2；k表示0或1至12；R.sup.1是氢、芳基、杂环、烷基、羟基或--OR.sup.7，其中R.sup.7是烷基、烯基或芳基烷基；A是--CON(R.sup.2)SO.sub.2--，其中R.sup.2是氢、烷基或芳基烷基；B是单键；以及其药学上可接受的盐。这些化合物具有增强谷胱甘肽还原酶活性的能力，因此可用于治疗和预防包括白内障在内的各种疾病。
• Solvent-Responsive Wettability of Self-Assembled Monolayers of Dithiooctanoic Acid Derivatives Bearing <i>N</i>,<i>N</i>-Disubstituted Amide Groups
  作者：Fangming Liu、Juan Pang、Chunyu Wang、Liyan Wang

  DOI：10.1021/la403442w

  日期：2013.10.22

  These films showed a reversible changes in wettability, one of which was indicated by surface contact angle switching between 40° and 59° upon alternating treatment with ethanol and cyclohexane. NMR experimental results of a model molecule suggest that the solvent-responsive wettability of the SAMs could be related with the changes in the relative populations of two stereoisomers of amide. The solvent

  我们设计并合成了两个带有N，N-二取代酰胺基的二硫代辛酸衍生物，并用它们在金表面上制备自组装单分子膜（SAMs）。这些薄膜显示出可润湿性的可逆变化，其中之一是在用乙醇和环己烷交替处理后，表面接触角在40°和59°之间切换。模型分子的NMR实验结果表明，SAMs的溶剂响应润湿性可能与酰胺的两种立体异构体的相对种群的变化有关。还研究了由其他两种酰胺制备的SAM的溶剂响应性，结果证实N，N-二取代对于含酰胺的SAM具有刺激反应性是必不可少的。因此，引入表现出受控的构象异构化的官能团可以是设计新的刺激响应材料的有效策略。
• PH-sensitive linkers for delivering a therapeutic agent
  申请人：GNT BIOTECH & MEDICALS CORPORATION

  公开号：US10688193B2

  公开（公告）日：2020-06-23

  The invention provides a pH-sensitive linker that can simultaneously bind metallic nanoparticles and one or more agents with various molecular size. The linker of the invention can deliver the agents into cells involved in disease processes or close to cells so that the agents can selectively target and effect on the cells. The target delivery provided by the linker of the invention can be used for example for disease sensing, imaging, drug delivery, and therapy.

  本发明提供了一种可同时结合金属纳米粒子和一种或多种不同分子大小的制剂的 pH 值敏感连接剂。本发明的连接剂可将药剂输送到涉及疾病过程的细胞或靠近细胞的地方，从而使药剂有选择地靶向作用于细胞。本发明的连接剂提供的靶向输送可用于疾病传感、成像、给药和治疗等。
• Organ/Cell-Selective Intracellular Delivery of Biologics via N-Acetylated Galactosamine-Functionalized Polydisulfide Conjugates
  作者：Jianhua Lu、Yuanhao Dai、Yahui He、Ting Zhang、Jing Zhang、Xiangmei Chen、Changtao Jiang、Hua Lu

  DOI：10.1021/jacs.3c11914

  日期：2024.2.14

  Biologics, including proteins and antisense oligonucleotides (ASOs), face significant challenges when it comes to achieving intracellular delivery within specific organs or cells through systemic administrations. In this study, we present a novel approach for delivering proteins and ASOs to liver cells, both in vitro and in vivo, using conjugates that tether N-acetylated galactosamine (GalNAc)-functionalized

  当通过全身给药在特定器官或细胞内实现细胞内递送时，包括蛋白质和反义寡核苷酸 (ASO) 在内的生物制剂面临着重大挑战。在这项研究中，我们提出了一种在体外和体内将蛋白质和 ASO 递送至肝细胞的新方法，使用连接N-乙酰化半乳糖胺 (GalNAc) 功能化、细胞穿透性聚二硫醚 (PDS) 的缀合物。该方法涉及通过所谓的聚集诱导聚合对 GalNAc 功能化的硫辛酰胺单体进行带有硫醇的货物介导的开环聚合，从而形成具有窄分散性的位点特异性蛋白质/ASO-PDS 缀合物。结合物的肝细胞选择性细胞内递送是由多种因素共同产生的，包括首先 GalNAc 与肝细胞上的 ASGPR 受体结合，导致细胞固定，以及随后在细胞表面发生的硫醇-二硫键交换，促进内化。我们的研究结果强调了 PDS 主链与细胞表面紧密相连的关键作用，因为它控制着硫醇-二硫键交换的成功，从而控制着细胞渗透。这些缀合物在克服生物大分子货物的系统
• Linker Compound, Ligand Conjugate, and Production Methods Thereof
  申请人：Suda Yasuo

  公开号：US20070213523A1

  公开（公告）日：2007-09-13

  The present invention provides a novel linker compound which minimizes any nonspecific hydrophobic interactions and is capable of easily adjusting the length to a disulfide group subjected to metal bond to thereby enable effective formation of a metal-sulfur bond; novel ligand conjugate and ligand carrier, and a process for producing them. The linker compound is of a structure represented by the following general formula (1) where a, b, d, e are independently an integer of 0 to 6. X has a structure serving as a multi-branched structure moiety including three or more hydrocarbon derivative chains, wherein the hydrocarbon derivative chains each include an aromatic amino group at an end thereof, and may or may not include a carbon-nitrogen bond in a main chain thereof. The ligand conjugate includes the linker compound having a sugar molecule introduced therein.