CN109221384A - 一种含吡咯化合物的应用 - Google Patents

一种含吡咯化合物的应用 Download PDF

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Publication number
CN109221384A
CN109221384A CN201811108556.7A CN201811108556A CN109221384A CN 109221384 A CN109221384 A CN 109221384A CN 201811108556 A CN201811108556 A CN 201811108556A CN 109221384 A CN109221384 A CN 109221384A
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Prior art keywords
hydrogen
azole compounds
application
containing azole
tyrosinase
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徐学涛
吕卉
黄丹颖
张焜
李冬利
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International Healthcare Innovation Institute (jiangmen)
Wuyi University
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International Healthcare Innovation Institute (jiangmen)
Wuyi University
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    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23B—PRESERVING, e.g. BY CANNING, MEAT, FISH, EGGS, FRUIT, VEGETABLES, EDIBLE SEEDS; CHEMICAL RIPENING OF FRUIT OR VEGETABLES; THE PRESERVED, RIPENED, OR CANNED PRODUCTS
    • A23B7/00—Preservation or chemical ripening of fruit or vegetables
    • A23B7/14—Preserving or ripening with chemicals not covered by groups A23B7/08 or A23B7/10
    • A23B7/153—Preserving or ripening with chemicals not covered by groups A23B7/08 or A23B7/10 in the form of liquids or solids
    • A23B7/154—Organic compounds; Microorganisms; Enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Microbiology (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Epidemiology (AREA)
  • Food Preservation Except Freezing, Refrigeration, And Drying (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

本发明公开了一种含吡咯化合物的应用，所述含吡咯化合物结构通式如式(Ⅰ)所示：

Description

一种含吡咯化合物的应用
技术领域
本发明涉及医药领域，具体涉及一种含吡咯化合物的新用途。
技术背景
酪氨酸酶广泛存在于动植物体，在动植物体内酶促褐变、体内色素合成的过程中起了关键的作用。它具有单酚酶的活性能将酪氨酸羟化，产生邻位二羟基苯丙氨酸(L-多巴)，也具有二酚酶的活性，能将L-多巴氧化成多巴醌，进而生成黑色素。酪氨酸酶抑制剂就是通过抑制酪氨酸酶活性从而抑制黑色素生成。此外，酪氨酸酶还是水果、蔬菜等水果发生褐变的关键原因，造成了食品质量的降低。当前市场常见酪氨酸酶抑制剂，包括：抗坏血酸衍生物、熊果苷和氢醌等，但其中许多化合物已经被证实对皮肤细胞有致变等毒性作用。因此，继续寻找和发现新型、高效且安全的酪氨酸酶抑制剂仍是当前研究的热点。
发明内容
本发明的目的在于提供一种含吡咯化合物在酪氨酸酶抑制剂和食品保鲜剂中的应用。
所述吡咯衍生物的结构通式如下：
其中：R1，R2，R3，R4可为氢、氟、氯、溴、甲氧基、乙烯基或三氟甲基；
所述含吡咯化合物在制备酪氨酸酶抑制剂中的应用。
所述含吡咯化合物在制备食品保鲜剂中的应用。
具体实施方式
为了更好的说明本发明的目的、技术方案和优点，下面将结合具体实施例对本发明进行说明。
实施例1
本实施例研究本发明所述含吡咯化合物抑制酪氨酸酶的作用。
将本发明的含吡咯化合物用DMSO溶解，配成2mmol/L的母液。在1ml塑料离心管中加入50μL待测化合物、50μL酪氨酸酶(浓度为666.6U/mL)与650μL磷酸盐缓冲溶液(浓度为50mmol/L)混合均匀，入250μL L-DOPA(浓度为1mmol/L)后在475nm波长下测定1分钟内吸光度的变化。以二甲基亚峰作为空白对照组。抑制活性＝[吸光度(空白)-吸光度(化合物)]/吸光度(空白)×100％。含吡咯化合物终浓度100μmol/L时抑制酪氨酸酶活性如表1所示：
表1含吡咯化合物在终浓度100μmol/L时抑制酪氨酸酶活性
化合物编号 R<sub>1</sub> R<sub>2</sub> R<sub>3</sub> R<sub>4</sub> 抑制率(％)
1 氢 氢 氢 氢 94
2 氟 氢 氢 氢 95
3 氢 氟 氢 氢 78
4 溴 氢 氢 氢 85
5 氢 溴 氢 氢 93
6 氢 氢 溴 氢 95
7 甲氧基 氢 氢 氢 75
8 氢 甲氧基 氢 氢 62
9 氢 三氟甲基 氢 氢 89
10 氯 氯 氢 氢 93
11 氢 溴 氢 甲氧基 98
12 乙烯基 氢 氢 氢 95
实施例2
本实施例研究本发明所述含吡咯化合物抑制酪氨酸酶的作用抑制酪氨酸酶的半数抑制浓度。
将化合物用DMSO配成不同浓度，参照实施例1中的方法测定不同浓度时化合物的抑制率，可求得化合物的半数抑制浓度。含吡咯化合物抑制酪氨酸酶的半数抑制浓度如表2所示：
表2含吡咯化合物在终浓度100μmol/L时抑制酪氨酸酶活性

Claims (3)

1.一种含吡咯化合物的应用，其特征在于，所述吡咯衍生物具有如下结构通式：
其中：R1，R2，R3，R4可为氢、氟、氯、溴、甲氧基、乙烯基或三氟甲基。
2.根据权利要求1所述一种含吡咯化合物的应用，其特征在于，所述应用为在制备酪氨酸酶抑制剂中的应用。
3.根据权利要求1所述一种含吡咯化合物的应用，其特征在于，所述应用为在制备食品保鲜剂中的应用。
CN201811108556.7A 2018-09-21 2018-09-21 一种含吡咯化合物的应用 Pending CN109221384A (zh)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1701069A (zh) * 2002-09-27 2005-11-23 詹森药业有限公司 3,4－二取代吡咯及其在治疗炎性疾病中的应用
CN107501156A (zh) * 2016-06-14 2017-12-22 兰州大学 一种多取代吡咯的三组分串联合成方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1701069A (zh) * 2002-09-27 2005-11-23 詹森药业有限公司 3,4－二取代吡咯及其在治疗炎性疾病中的应用
CN107501156A (zh) * 2016-06-14 2017-12-22 兰州大学 一种多取代吡咯的三组分串联合成方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
XUE-QING MOU等: "The Synthesis of Multisubstituted Pyrroles via a Copper-Catalyzed Tandem Three-Component Reaction", 《ORGANIC LETTERS》 *

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