N-propionyl-L-valine | 20051-64-3

• 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
• 英文名称: N-propionyl-L-valine
• 英文别名: propionyl-Val-OH；propionyl-L-valine；(2S)-3-methyl-2-(propanoylamino)butanoic acid
• CAS: 20051-64-3
• 化学式: C₈H₁₅NO₃
• 分子量: 173.212
• InChiKey: ONFCFBRYSUZTJY-ZETCQYMHSA-N

物化性质

• 熔点：
  199.5-201.5 °C
• 沸点：
  369.7±25.0 °C(Predicted)
• 密度：
  1.069±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  66.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-propionyl-L-valine 在 4-二甲氨基吡啶 、 1-羟基苯并三唑 、 戴斯-马丁氧化剂 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三氟乙酸 作用下， 生成 5-Fluoro-3-((S)-3-methyl-2-propionylamino-butyrylamino)-4-oxo-pentanoic acid
  参考文献：
  名称：

  Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group

  摘要：

  This article describes the synthesis and biological evaluation of a group of N-protected Val-Asp-fmk as caspase inhibitors. The protecting group was found to contribute to caspase-3 inhibiting activity, and compounds with a large group such as Cbz are more active than compounds with a small group such as Ac. Compounds with more hydrophobic protecting groups were found to be more active in cell apoptosis protection assays, probably due to increased cell permeability. MX1122,2,4-di-Cl-Cbz-Val-Aspfmk, is identified as a potent broad-spectrum caspase inhibitor and is selective for caspases versus other proteases, with good activity in the cell apoptosis protection assays as well as good efficacy in the mouse liver apoptosis model. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.08.027
• 作为产物：
  描述：

  silver L-valinate 、 丙酰氯 生成 N-propionyl-L-valine
  参考文献：
  名称：

  ZAXARIEV, SOTIR GEORGIEV;STOEV, STOJCHO BORISOV;GOLOVINSKI, EVGENI VIKTOR+

  摘要：

  DOI：

文献信息

• PDE 10a Inhibitors for the Treatment of Type II Diabetes
  申请人：Janssen Pharmaceutica, NV

  公开号：US20140364414A1

  公开（公告）日：2014-12-11

  Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: wherein R 1 , R 2 , L, and Q are defined herein.

  揭示了用于治疗2型糖尿病的化合物、组合物和方法。这些化合物由以下式（I）表示： 其中R1、R2、L和Q在此处定义。
• ANTIVIRAL COMPOUNDS
  申请人：Guo Hongyan

  公开号：US20120264711A1

  公开（公告）日：2012-10-18

  The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

  该发明涉及抗病毒化合物、含有这种化合物的组合物、包括给予这种化合物的治疗方法，以及用于制备这种化合物的过程和中间体。
• TETRAHYDROISOQUINOLINE DERIVATIVE, PREPARATION METHOD THEREFOR AND USES THEREOF
  申请人：Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.

  公开号：EP3778597A1

  公开（公告）日：2021-02-17

  Provided are tetrahydroisoquinoline derivatives, the preparation and use thereof. More specifically, provided are the tetrahydroisoquinoline derivatives or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, polymorph, solvate, isotopically labeled compound, metabolite or prodrug thereof. Further provided are a preparation process of the compound, the intermediates, a pharmaceutical composition comprising the compound and the use thereof in the treatment or prevention of a thromboembolic disorder.

  本发明提供了四氢异喹啉衍生物及其制备方法和用途。更具体地说，提供了四氢异喹啉衍生物或其药学上可接受的盐、酯、立体异构体、同分异构体、多晶型、溶解物、同位素标记化合物、代谢物或原药。进一步提供了该化合物的制备工艺、中间体、包含该化合物的药物组合物及其在治疗或预防血栓栓塞性疾病中的用途。
• ARF6 inhibitors and related methods
  申请人：Navigen, Inc.

  公开号：US11414442B2

  公开（公告）日：2022-08-16

  Methods of treating vascular leak, vascular inflammation, angiogenesis, ocular disorders, and/or inflammatory disorders in a patient are provided. The methods can include administering an ADP-ribosylation factor 6 (ARF6) inhibitor to the patient. The present disclosure also relates to new chemical entities and pharmaceutical compositions including ARF6 inhibitors. The ARF6 inhibitor may be a prodrug of an ARF6 inhibitor.

  提供了治疗患者血管渗漏、血管炎症、血管生成、眼部疾病和/或炎症性疾病的方法。这些方法可包括向患者施用 ADP- 核糖基化因子 6 (ARF6) 抑制剂。本公开还涉及包括 ARF6 抑制剂的新化学实体和药物组合物。ARF6抑制剂可以是ARF6抑制剂的原药。
• Enlargement of mucocutaneous or cutaneous organs and sites with topical compositions
  申请人：Yu J. Ruey

  公开号：US20050171194A1

  公开（公告）日：2005-08-04

  Compositions comprising a hydroxycarboxylic acid, N-acyl-aldosamine, N-acylamino acid or related compound on topical application are beneficial to plump and pout lips, enhance and firm eyelids, enlarge and augment breasts, elongate and expand penis. Because of antioxidant property, certain hydroxycarboxylic acids, N-acyl-aldosamines, N-acylamino acids and related compounds also are useful for topical administration to prevent occurrence of breast cancer or other forms of tumors and cancers.

  由羟基羧酸、N-酰基-醛糖胺、N-酰基氨基酸或相关化合物组成的组合物在局部使用时有利于丰满嘴唇、增强和紧实眼睑、增大和隆起乳房、拉长和扩张阴茎。由于具有抗氧化性，某些羟基羧酸、N-酰基醛胺和 N-酰基氨基酸及相关化合物还可用于局部用药，以预防乳腺癌或其他形式的肿瘤和癌症的发生。