乙基-L-噻唑烷-4-羧酸酯 | 14347-73-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 乙基-L-噻唑烷-4-羧酸酯
• 中文别名: 2-乙基噻唑烷-4-羧酸；L-噻唑啉-4甲酸乙酯
• 英文名称: 2-ethylthiazolidine-4-carboxylic acid
• 英文别名: 2-Aethyl-thiazolidin-4-carbonsaeure；2-Ethylthiazolidin-4-carbonsaeure；N,S-propane-1,1-diyl-cysteine；2-ethyl-4-thiazolidinecarboxylic acid；2-ethyl-1,3-thiazolidin-3-ium-4-carboxylate
• CAS: 14347-73-0
• 化学式: C₆H₁₁NO₂S
• mdl: MFCD27756510
• 分子量: 161.225
• InChiKey: RSZVGLFPGDKTDK-UHFFFAOYSA-N

物化性质

• 沸点：
  338.2±37.0 °C(Predicted)
• 密度：
  1.202±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  74.6
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  3-乙酰硫基-2-甲基丙酰氯 、 乙基-L-噻唑烷-4-羧酸酯 在 ice water 、 乙醚 、 乙酸乙酯 、 magnesium sulfate 作用下， 以 sodium hydroxide 为溶剂， 反应 3.0h， 以to yield 3-(3-acetylthio-2-methylpropanoyl)-2-ethyl-4-thiazolidinecarboxylic acid的产率得到3-(3-acetylthio-2-methylpropanoyl)-2-ethyl-4-thiazolidinecarboxylic acid
  参考文献：
  名称：

  Derivatives of thiazolidinecarboxylic acids and related acids

  摘要：

  新的取代硫唑啉、硫唑烷和相关羧酸衍生物，其通式为##STR1##，可用作血管紧张素转换酶抑制剂。

  公开号：

  US04237134A1

文献信息

• [EN] IMPROVED PEPTIDYL CALCINEURIN INHIBITORS<br/>[FR] INHIBITEURS AMÉLIORÉS DE LA PEPTIDYL-CALCINEURINE
  申请人：OHIO STATE INNOVATION FOUNDATION

  公开号：WO2016033368A1

  公开（公告）日：2016-03-03

  Improved calcineurin inhibitors and methods of using these improved calcineurin inhibitors to inhibit calcineurin-NFAT signaling in cells and in subjects are disclosed.

  揭示了改良的钙调神经酰胺酶抑制剂及其在细胞和受试者中用于抑制钙调神经酰胺酶-NFAT信号的方法。
• Pharmaceutical composition for tumour treatment and process for preparing it
  申请人：NATIONAL FOUNDATION FOR CANCER RESEARCH, INC.

  公开号：EP0060659A1

  公开（公告）日：1982-09-22

  An adduct of glyoxal and cysteine containing free radicals is a valuable vehicle for transporting glyoxal (known to have anti-tumour activity) to the tumour site, without interference from the body chemistry. The adduct may be prepared by reacting glyoxal and cysteine in solution and exposing the reaction product to oxygen, preferably by carrying out the reaction under vigorous oxygenation. The adduct may be formulated with conventional pharmaceutical carriers and diluents to prepare a pharmaceutical composition for parenteral or oral use.

  乙二醛和含有自由基的半胱氨酸的加合物是将乙二醛（已知具有抗肿瘤活性）运送到肿瘤部位的重要载体，而不会受到体内化学物质的干扰。加合物可以通过乙二醛和半胱氨酸在溶液中反应，并将反应产物暴露于氧气中来制备，最好是在剧烈充氧的情况下进行反应。加合物可与常规药物载体和稀释剂配制成用于肠外或口服的药物组合物。
• Microorganisms and process for the production of riboflavin by fermentation
  申请人：CJ Corporation

  公开号：EP1426450A1

  公开（公告）日：2004-06-09

  Riboflavin-producing Bacillus subtilis which is resistant to proline analogue, and a method for producing riboflavin using the Bacillus subtilis are provided.

  提供了对脯氨酸类似物具有抗性的核黄素生产枯草芽孢杆菌，以及利用该枯草芽孢杆菌生产核黄素的方法。
• Substrates and inhibitors of prolyl oligopeptidase and methods of use thereof
  申请人：The Board of Regents of the University of Oklahoma

  公开号：US10155789B2

  公开（公告）日：2018-12-18

  Inhibitors of fibroblast activation protein alpha (FAP) and Prolyl Oligopeptidase (POP) are disclosed, along with their use in various therapies related to conditions, diseases, and disorders involving abnormal cell proliferation such as malignancies and angiogenesis, and in neural disorders such as Alzheimer's disease. Stalk portions of the inhibitor molecules, and substrates of FAP and POP, are also disclosed and may be used, for example, in screening methods for identifying such inhibitors.

  本研究公开了成纤维细胞活化蛋白α（FAP）和脯氨酰寡肽酶（POP）的抑制剂，以及它们在涉及异常细胞增殖（如恶性肿瘤和血管生成）的条件、疾病和紊乱以及神经紊乱（如阿尔茨海默病）的各种疗法中的用途。此外，还公开了抑制剂分子的柄部分以及 FAP 和 POP 的底物，例如，可用于识别此类抑制剂的筛选方法。
• Method of inhibiting activity of cell surface fibroblast activation protein alpha
  申请人：The Board of Regents of the University of Oklahoma

  公开号：US10174077B2

  公开（公告）日：2019-01-08

  The presently disclosed inventive concept(s) include inhibitors of antiplasmin cleaving enzyme (APCE) and fibroblast activation protein alpha (FAP) which can be used in various therapies related to disorders of fibrin and α2-antiplasmin and abnormal cell proliferation. The presently disclosed inventive concept(s) also include substrates of APCE and FAP, which may be used, for example, in screening methods for identifying such inhibitors. The presently disclosed inventive concept(s) further include, but are not limited to, methods of treating or inhibiting atherosclerosis and thrombus disorders by altering the ratios of types of plasma α2-antiplasmin and to methods of treating conditions involving abnormal cell proliferation such as cancers.

  本发明公开的发明概念包括抗蛋白溶解酶（APCE）和成纤维细胞活化蛋白α（FAP）的抑制剂，这些抑制剂可用于与纤维蛋白和α2-抗蛋白溶解酶紊乱以及异常细胞增殖有关的各种治疗中。本发明公开的发明构思还包括 APCE 和 FAP 的底物，例如，可用于鉴定此类抑制剂的筛选方法中。目前公开的发明概念还包括但不限于通过改变血浆α2-抗蛋白酶类型的比例来治疗或抑制动脉粥样硬化和血栓疾病的方法，以及治疗涉及异常细胞增殖（如癌症）的病症的方法。