4-(3-吲哚)-dl-beta-高丙氨酸 | 2474-01-3

• 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: 4-(3-吲哚)-dl-beta-高丙氨酸
• 英文名称: tryptophan
• 英文别名: 3-(2-Amino-3-carboxy-propyl)-indol；3-Amino-4-indolyl-(3)-buttersaeure；3-amino-4-indol-3-yl-butyric acid；3-azaniumyl-4-(1H-indol-3-yl)butanoate
• CAS: 2474-01-3
• 化学式: C₁₂H₁₄N₂O₂
• 分子量: 218.255
• InChiKey: DUVVFMLAHWNDJD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  79.1
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  4-(3-吲哚)-dl-beta-高丙氨酸 、 螺谷胺 在 氯甲酸乙酯 、 三乙胺 作用下， 生成 3-[[(4R)-5-(8-azaspiro[4.5]decan-8-yl)-4-[(3,5-dichlorobenzoyl)amino]-5-oxopentanoyl]amino]-4-(1H-indol-3-yl)butanoic acid
  参考文献：
  名称：

  Structure−Antigastrin Activity Relationships of New Spiroglumide Amido Acid Derivatives

  摘要：

  A series of new spiroglumide amido acid derivatives was synthesized and evaluated for their ability to inhibit the binding of cholecystokinin (CCK) to guinea pig brain cortex (CCKB receptors) and peripheral rat pancreatic acini (CCKA receptors), as well as to inhibit in vitro the gastrin-induced Ca2+ increase in rabbit gastric parietal cells. Appropriate chemical manipulations of the structure of spiroglumide (CR 2194), i.e., (R)-4-(3,5-dichlorobenzamido)-5-(8-azaspiro[4,5]decan-8-yl)-5-oxopentanoic acid, led to potent and selective antagonists of CCKB/gastrin receptors. Structure-activity relationships are discussed. Some of these new derivatives, as, for example, compound 54 (CR 2622), i.e., (S)-4-[[(R)-4'-[(3,5-dichlorobenzoyl)amino]-5'-(8-azaspiro[4.5] decan-8-yl)-5'-oxo-pentanonyl]amino]-5-(1-naphthylamino)-5- oxopentanoic acid, exhibit activity 70-170 times greater than that of spiroglumide, depending upon the model used (IC50 = 2 x 10(-8) vs 140 x 10(-8) mol in binding inhibition of [H-3]-N-Me-N-Leu-CCK-8 in guinea pig brain cortex and IC50 = 0.7 x 10(-8) vs 122.3 x 10(-8) mol in inhibition of gastrin-induced Ca2+ mobilization in parietal cells of rabbit, respectively). Computer-assisted conformational analysis studies were carried out in order to compare the chemical structure of both the agonist (pentagastrin) and the antagonist (54).

  DOI：

  10.1021/jm950372w

文献信息

• Endothelin antagonistic peptide derivatives
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：EP0460679A2

  公开（公告）日：1991-12-11

  1. A peptide derivative of the formula:

  1.式中的肽衍生物：
• Novel depsipeptides and process for preparing same
  申请人：Cubist Pharmaceutical Inc.

  公开号：EP1932853A1

  公开（公告）日：2008-06-18

  The present invention relates to novel depsipeptide compounds. The invention also relates to pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The invention also relates to methods of producing these novel depsipeptide compounds and imntermediates used in producing these compounds.

  本发明涉及新型去肽化合物。本发明还涉及这些化合物的药物组合物以及将这些化合物用作抗菌化合物的方法。本发明还涉及生产这些新型去肽化合物的方法和用于生产这些化合物的中间体。
• Tissue protective peptides for preventing and treating diseases and disorders associated with tissue damage
  申请人：Araim Pharmaceuticals, Inc.

  公开号：US10864253B2

  公开（公告）日：2020-12-15

  Provided herein are peptides and peptide analogs that have tissue protective activities. The peptides and peptide analogs are useful in preventing and treating a variety of diseases and disorders associated with tissue damage.

  本文提供了具有组织保护活性的肽和肽类似物。这些肽和肽类似物可用于预防和治疗与组织损伤有关的各种疾病和失调。
• WHOLE CELL BIOCATALYST COMPRISING A PRENYLTRANSFERASE
  申请人：Autodisplay Biotech GmbH

  公开号：EP2707482B1

  公开（公告）日：2015-09-09
• Novel Depsipeptides and Process for Preparing Same
  申请人：Finn John

  公开号：US20080119395A1

  公开（公告）日：2008-05-22

  The present invention relates to novel depsipeptide compounds. The invention also relates to pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The invention also relates to methods of producing these novel depsipeptide compounds and intermediates used in producing these compounds.