2-(2-Carboxy-ethylmercapto)-pyridin | 32002-84-9

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 英文名称: 2-(2-Carboxy-ethylmercapto)-pyridin
• 英文别名: 3-(Pyridin-2-ylsulfanyl)propanoic acid；3-pyridin-2-ylsulfanylpropanoic acid
• CAS: 32002-84-9
• 化学式: C₈H₉NO₂S
• mdl: MFCD02929354
• 分子量: 183.231
• InChiKey: WXKRKQBCEWPFLB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  75.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] PYRIDIN- 2 - YL SULFANYL ACID ESTERS AND PROCESS FOR THE PREPARATION THEREOF<br/>[FR] ESTERS DE PYRIDIN-2-YLSULFANYLACIDES ET LEUR PROCÉDÉ DE SYNTHÈSE
  申请人：COUNCIL SCIENT IND RES

  公开号：WO2012011123A1

  公开（公告）日：2012-01-26

  The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HUVEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS-Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure la, R1 = H, R2 = H, R3 = CH2COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.

  本发明涉及具有抗炎性质的吡啶-2-基巯酸酯化合物。本发明特别涉及一类新型的抗炎杂环酸酯，其具有通用公式1的结构，并且已经通过抑制从人外周血中分离的中性粒细胞粘附到人脐静脉内皮细胞（HUVEC）表面的能力来筛选其抗炎活性，这是通过抑制细胞粘附分子ICAM-1的细胞因子刺激表达的结果。发现化合物RS-Z，3-(吡啶-2-基巯基)-丙酸戊酯（结构la，R1 = H，R2 = H，R3 = CH2COOC5H11）对ICAM-1和中性粒细胞粘附抑制最有效，并且发现它有效地缓解了由过度白细胞浸润导致的炎症介导的炎症疾病或类似状况，例如小鼠的急性肺损伤和急性呼吸窘迫综合征。
• Compositions and methods for treatment of neoplastic disease
  申请人：——

  公开号：US20020177551A1

  公开（公告）日：2002-11-28

  The present invention comprises compositions and methods for treating a tumor or neoplastic disease in a host, The methods employ conjugates comprising superantigen polypeptides, nucleic acids with other structures that preferentially bind to tumor cells and are capable of inducing apoptosis. Also provided are superantigen-glycolipid conjugates and vesicles that are loaded onto antigen presenting cells to activate both T cells and NKT cells. Cell-based vaccines comprise tumor cells engineered to express a superantigen along with glycolipids products which, when expressed, render the cells capable of eliciting an effective anti-tumor immune response in a mammal into which these cells are introduced. Included among these compositions are tumor cells, hybrid cells of tumor cells and accessory cells, preferably dendritic cells. Also provided are tumoricidal T cells and NKT cells devoid of inhitory receptors or inhibitory signaling motifs which are hyperresponsive to the the above compositions and lipid-based tumor associated antigens that can be administered for adoptive immunotherapy of cancer and infectious diseases.

  本发明涉及一种用于治疗宿主体内肿瘤或肿瘤性疾病的组合物和方法。该方法采用包含超抗原多肽、具有其他结构的核酸和优先结合于肿瘤细胞并能够诱导细胞凋亡的结构的共轭物。还提供了超抗原-糖脂共轭物和负载于抗原呈递细胞上的囊泡，以激活T细胞和NKT细胞。基于细胞的疫苗包括肿瘤细胞，这些肿瘤细胞被改造以表达超抗原和糖脂产物，当这些细胞被引入哺乳动物体内时，这些细胞能够引起有效的抗肿瘤免疫反应。这些组合物包括肿瘤细胞、肿瘤细胞和辅助细胞的杂交细胞，优选为树突状细胞。还提供了无抑制性受体或抑制性信号基序的肿瘤细胞杀伤T细胞和NKT细胞，这些细胞对上述组合物和基于脂质的肿瘤相关抗原具有高度反应性，可用于癌症和传染病的免疫治疗。
• Peridinin-chlorophyll complex as fluorescent label
  申请人：Becton Dickinson and Company

  公开号：EP0314406A1

  公开（公告）日：1989-05-03

  Peridinin-chlorophyll-protein complexes are provided for use as fluorescent labels and are particu­larly useful in diagnostic assays employing as a rea­gent a fluorescent compound conjugated to a member of a specific binding pair, wherein the pair consists of a biochemical ligand and a receptor and the diagnostic assay comprises a step in which the conjugate binds to its complementary binding-pair member.

  荧光素-叶绿素-蛋白质复合物可用作荧光标记，尤其适用于诊断分析，其试剂是与特定结合对成员结合的荧光化合物，其中结合对由生化配体和受体组成，诊断分析包括一个步骤，在该步骤中，共轭物与其互补的结合对成员结合。
• Rhizoxin derivates and their use as anti-tumor agents
  申请人：SANKYO COMPANY LIMITED

  公开号：EP0350315A1

  公开（公告）日：1990-01-10

  Rhizoxin and rhizoxin-2-ene derivatives of formula (I): [in which: n is 1 to 25; A is an extra bond or oxygen, X is oxygen, sulphur, nitrogen or carbonyl; and R is hydrogen, carboxylic acyl having from 1 to 25 carbon atoms, alkoxycarbonyl group having from 2 to 26 carbon atoms, phosphono, alkylphosphono group in which the alkyl part has from 1 to 25 carbon atoms, dialkyl­phosphono group in which each alkyl part has from 1 to 25 carbon atoms, alkyl group having from 1 to 25 carbon atoms, aralkyl, cycloalkyl, heterocyclic, alkylthio group in which the alkyl part has from 1 to 25 carbon atoms, aralkylthio, or heterocyclylthio, or when X represents a nitrogen atom, R is R¹ and R², where R¹ and R² are hydrogen, alkyl, acyl, alkoxycarbonyl, phosphono, alkylphosphono or dialkylphosphono] have valuable anti-tumour activity. They may be prepared by acylation of rhizoxin or rhizoxin-2-ene.

  式(I)的根肿灵和根肿灵-2-烯衍生物： 其中n 为 1 至 25；A 为额外键或氧，X 为氧、硫、氮或羰基；和 R 是氢、具有 1 至 25 个碳原子的羧酰基、具有 2 至 26 个碳原子的烷氧羰基、膦酰基、烷基膦酰基（其中烷基部分具有 1 至 25 个碳原子）、二烷基膦酰基（其中每个烷基部分具有 1 至 25 个碳原子）、具有 1 至 25 个碳原子的烷基、或当 X 代表氮原子时，R 为 R¹ 和 R²，其中 R¹ 和 R²为氢、烷基、酰基、烷氧羰基、膦酰基、烷基膦酰基或二烷基膦酰基]具有重要的抗肿瘤活性。它们可通过 rhizoxin 或 rhizoxin-2-ene 的酰化反应制备。
• Detection of antibiotics
  申请人：GIST-BROCADES N.V.

  公开号：EP0593112A1

  公开（公告）日：1994-04-20

  A process for the detection of antibiotics in a liquid medium such as milk, urine and blood is disclosed which comprises bringing together a fluid sample of the liquid medium, an labelled antibiotic binding protein, and an immobilized antibiotic, allowing the labelled antibiotic binding protein to bind with the immobilized antibiotic, removing labelled antibiotic binding protein which is not bound to immobilized antibiotic, and determining the amount of the labelled antibiotic binding protein bound to the immobilized antibiotic.

  本发明公开了一种检测牛奶、尿液和血液等液体介质中抗生素的方法，该方法包括 将液体介质的液体样品、标记的抗生素结合蛋白和固定化抗生素放在一起、 让标记的抗生素结合蛋白与固定化抗生素结合、 去除未与固定化抗生素结合的标记抗生素结合蛋白，以及 确定与固定化抗生素结合的标记抗生素结合蛋白的量。