(R)-(-)-3-(4-Phenylbutanoyl)thiazolidine-4-carboxylic acid | 122230-47-1

• 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: (R)-(-)-3-(4-Phenylbutanoyl)thiazolidine-4-carboxylic acid
• 英文别名: N-(4-phenylbutanoyl)-L-thioproline；(4R)-3-(4-phenylbutanoyl)-1,3-thiazolidine-4-carboxylic acid
• CAS: 122230-47-1
• 化学式: C₁₄H₁₇NO₃S
• mdl: MFCD16379411
• 分子量: 279.36
• InChiKey: NLKSPDZPJKTOEB-LBPRGKRZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.428
• 拓扑面积：
  82.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R)-(-)-3-(4-Phenylbutanoyl)thiazolidine-4-carboxylic acid 生成 3-[(R)-(-)-3-(4-Phenylbutanoyl)thiazolidine-4-carbonyl]thiazolidine
  参考文献：
  名称：

  FURUKAVA, ATSUSI;JOSIMOTO, TADASI;ADZISAVA, KOESI;IKEHGUTI, SEHJITI;KISIT+

  摘要：

  DOI：
• 作为产物：
  描述：

  L-硫代脯氨酸 生成 (R)-(-)-3-(4-Phenylbutanoyl)thiazolidine-4-carboxylic acid
  参考文献：
  名称：

  FURUKAVA, ATSUSI;JOSIMOTO, TADASI;ADZISAVA, KOESI;IKEHGUTI, SEHJITI;KISIT+

  摘要：

  DOI：

文献信息

• Synthesis of Prolyl Endopeptidase Inhibitors and Evaluation of Their Structure-Activity Relationships: In Vitro Inhibition of Prolyl Endopeptidase from Canine Brain.
  作者：Heihachiro ARAI、Hiroyasu NISHIOKA、Seiichi NIWA、Takeshi YAMANAKA、Yoshiaki TANAKA、Koji YOSHINAGA、Naomi KOBAYASHI、Naoyoshi MIURA、Yugo IKEDA

  DOI：10.1248/cpb.41.1583

  日期：——

  By chemical modification of a known prolyl endopeptidase (PEP) inhibitor (N-[N-(4-phenylbutanoyl)-L-prolyl]pyrrolidine; SUAM-1221), several arylalkanoyl derivatives (V-1-27) were synthesized and tested for in vitro inhibitory activity towards PEP from canine brain. Among them, 4-(2-thienyl)butanoyl derivatives (V-24-27) showed more potent PEP-inhibitory activity than SUAM-1221. The structure-activity relationships of these compounds are discussed.

  通过对一种已知的脯氨酰内肽酶（PEP）抑制剂（N-[N-（4-苯基丁酰基）-L-脯氨酰]吡咯烷；SUAM-1221）进行化学修饰，合成了几种芳基烷酰基衍生物（V-1-27），并测试了其对犬脑中 PEP 的体外抑制活性。其中，4-（2-噻吩基）丁酰衍生物（V-24-27）显示出比 SUAM-1221 更强的 PEP 抑制活性。本文讨论了这些化合物的结构-活性关系。
• Amino acid imide derivatives, usage thereof, and medicinal composition
  申请人：Zeria Pharmaceutical Co., Ltd.

  公开号：US04916146A1

  公开（公告）日：1990-04-10

  Novel N-substituted amino acid imide derivatives are disclosed. The compounds are represented by formula (I): ##STR1## wherein n represents an integer of 0 to 5, and X and Y, which may be the same or different, represent a methylene group or a sulfur atom, provided that not both X and Y are methylene groups at the same time. The compounds are useful as a medicine for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance.

  本发明揭示了一种新型的N-取代氨基酸亚酰衍生物。该化合物的化学式为(I)：##STR1## 其中n表示0到5之间的整数，X和Y可以相同也可以不同，分别代表亚甲基基团或硫原子，但不能同时为亚甲基基团。该化合物可用作治疗或预防脑循环障碍、脑代谢障碍或记忆障碍的药物。
• Cholinesterase activator
  申请人：Zeria Pharmaceutical Co., Ltd.

  公开号：US06017929A1

  公开（公告）日：2000-01-25

  The invention relates to a cholinesterase activator comprising, as an active ingredient, a compound represented by the following general formula (I): ##STR1## wherein A means a group such as a phenyl group or indanyl group, B denotes a group such as a prolyl group or thioprolyl group, and m stands for an integer of 0-5. The cholinesterase activator according to the invention has a strongly activating action on cholinesterase, in particular, a selectively activating action on peripheral cholinesterase and is also high in safety. It is hence useful as an agent for preventing and treating the side effects of central cholinesterase inhibitors, in particular, hepatopathy, and an agent for preventing and treating the side effects of various medicines manifested on the basis of a cholinesterase-inhibiting action.

  本发明涉及一种胆碱酯酶激活剂，其包括以下通式(I)所表示的化合物作为活性成分：其中，A代表苯基或吲哚基等基团，B代表丙氨酸基或硫丙氨酸基等基团，m为0-5的整数。本发明中的胆碱酯酶激活剂对胆碱酯酶具有强烈的激活作用，特别是对周围胆碱酯酶具有选择性的激活作用，并且具有较高的安全性。因此，它可用作预防和治疗中枢胆碱酯酶抑制剂的副作用，特别是肝病的药物和预防和治疗基于胆碱酯酶抑制作用的各种药物的副作用的药物。
• Thiazolidine compounds
  申请人：Kissei Pharmaceutical Co Ltd

  公开号：EP0303434A1

  公开（公告）日：1989-02-15

  Thiazolidine compounds of the general formula: wherein Ar represents a phenyl group, a naphthyl group or a pyridyl group, Y represents a saturated or unsaturated alkylene group having 1 to 5 carbon atoms, n represents zero or 1, represents a 5- or 6-membered saturated heterocyclic group which may contain a hetero atom other than the nitrogen atom, X represents an oxygen atom, m represents zero or 1, R represents a hydrogen atom or an alkoxycarbonyl group; and pharmaceutically acceptable salts thereof, possess an inhibitory effect for prolyl endopeptidase, and are useful as therapeutical agents for the treatment of dementia and amnesia.

  通式如下的噻唑烷化合物 其中 Ar 代表苯基、萘基或吡啶基，Y 代表具有 1 至 5 个碳原子的饱和或不饱和亚 烷基，n 代表 0 或 1、 代表 5 或 6 元饱和杂环基团，该杂环基团可含有除氮原子之外的杂原子；X 代表氧原子；m 代表 0 或 1；R 代表氢原子或烷氧羰基；以及它们的药学上可接受的盐类，具有抑制脯氨酰内肽酶的作用，可用作治疗痴呆症和健忘症的治疗剂。
• TANAKA, JOSIAKI;AOTSUKA, TOMOSI;NAKADA, NAOKI;OGURA, KUNIESI;TORITSUKA, M+
  作者：TANAKA, JOSIAKI、AOTSUKA, TOMOSI、NAKADA, NAOKI、OGURA, KUNIESI、TORITSUKA, M+

  DOI：——

  日期：——