(2R)-1-[(naphthalen-1-yl)methyl]pyrrolidine-2-carboxylic acid

• 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
• 英文名称: (2R)-1-[(naphthalen-1-yl)methyl]pyrrolidine-2-carboxylic acid
• 英文别名: 1-(naphthalen-1-ylmethyl)pyrrolidine-2-carboxylic acid
• 化学式: C₁₆H₁₇NO₂
• mdl: MFCD12464855
• 分子量: 255.316
• InChiKey: MVPZPEPHGNXNOU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.312
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (2R)-1-[(naphthalen-1-yl)methyl]pyrrolidine-2-carboxylic acid 、 苯乙炔 在 copper (II) carbonate hydroxide 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 甲苯 为溶剂， 反应 24.0h， 以61%的产率得到1-(naphthalen-1-ylmethyl)-2-(phenylethynyl)pyrrolidine
  参考文献：
  名称：

  元素硫结合的吡咯烷并噻吩并吡咯类化合物的环化反应。

  摘要：

  我们在本文中报道了2-炔基吡咯烷与元素硫的直接氧化[4 + 1]环化反应合成噻吩并[3,2- b ]吡咯。该转变可能源自吡咯烷在β-位的亲电攻击，随后是分子内的噻吩环化以递送所需的产物。机理研究表明，该反应涉及二氢噻吩并[3，2- b ]吡咯作为中间体的形成。

  DOI：

  10.1021/acs.joc.0c01363

文献信息

• 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。
• Acceleration of Mycobacterium growth
  申请人：ST GEORGE'S HOSPITAL MEDICAL SCHOOL

  公开号：US10633630B2

  公开（公告）日：2020-04-28

  The invention is in the field of growth of Mycobacteria. In particular, agents have been identified which enhance the growth of Mycobacterial species, which are naturally slow-growing. Such agents can therefore be used in the identification of Mycobacteria and in the diagnosis of Mycobacterial infections.

  本发明属于分枝杆菌生长领域。特别是，已经发现了能促进自然生长缓慢的分枝杆菌生长的制剂。因此，这些制剂可用于分枝杆菌的鉴定和分枝杆菌感染的诊断。
• SMALL CATIONIC ANTIMICROBIAL PEPTIDES
  申请人：THE UNIVERSITY OF BRITISH COLUMBIA

  公开号：EP2061886A1

  公开（公告）日：2009-05-27
• EP2061886B1
  申请人：——

  公开号：EP2061886B1

  公开（公告）日：2014-05-07