• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

查耳酮及其吡唑衍生物的合成及血管紧张素转化酶（ACE）抑制活性。

The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives.

机构信息

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Nutrition and Health Sciences, University of Calabria, Rende (CS), Italy.

出版信息

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1990-3. doi: 10.1016/j.bmcl.2010.01.113. Epub 2010 Jan 25.

DOI:10.1016/j.bmcl.2010.01.113
PMID:20167484
Abstract

A series of chalcones (1-9) and pyrazoles (10-18) was prepared to investigate their potential activity as Angiotensin I-Converting Enzyme (ACE) inhibitors. Their structures were verified by elemental analysis, UV, IR, MS, (1)H NMR, (13)C NMR, and 2D NMR experiments. Among tested compounds, chalcone 7 exerted the highest activity with an IC(50) value of 0.219 mM, while the most potent pyrazole was 15 (IC(50) value of 0.213 mM).

摘要

我们合成了一系列查耳酮（1-9）和吡唑（10-18）衍生物，以研究它们作为血管紧张素转化酶（ACE）抑制剂的潜力。通过元素分析、紫外光谱、红外光谱、质谱、（1）H NMR、（13）C NMR 和二维 NMR 实验对它们的结构进行了验证。在所测试的化合物中，查尔酮 7 的活性最高，IC（50）值为 0.219mM，而最有效的吡唑衍生物是 15（IC（50）值为 0.213mM）。

相似文献

1
The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives.查耳酮及其吡唑衍生物的合成及血管紧张素转化酶（ACE）抑制活性。
Bioorg Med Chem Lett. 2010 Mar 15;20(6):1990-3. doi: 10.1016/j.bmcl.2010.01.113. Epub 2010 Jan 25.
2
Synthesis and evaluation of novel 2-butyl-4-chloro-1-methylimidazole embedded chalcones and pyrazoles as angiotensin converting enzyme (ACE) inhibitors.新型 2-丁基-4-氯-1-甲基咪唑嵌入查耳酮和吡唑类血管紧张素转化酶（ACE）抑制剂的合成与评价。
Bioorg Med Chem. 2011 Aug 15;19(16):4772-81. doi: 10.1016/j.bmc.2011.06.085. Epub 2011 Jul 2.
3
Synthesis, structure, and in vitro antitumor activity of some glycoside derivatives of ferrocenyl-chalcones and ferrocenyl-pyrazolines.二茂铁基查尔酮和二茂铁基吡唑啉的一些糖苷衍生物的合成、结构及体外抗肿瘤活性
ChemMedChem. 2006 Oct;1(10):1119-25. doi: 10.1002/cmdc.200600052.
4
Novel chalcones and 1,3,5-triphenyl-2-pyrazoline derivatives as antibacterial agents.新型查尔酮和 1,3,5-三苯基-2-吡唑啉衍生物作为抗菌剂。
Chem Biol Drug Des. 2010 Nov;76(5):407-11. doi: 10.1111/j.1747-0285.2010.01020.x.
5
Synthesis and biological evaluation of a novel series of chalcones incorporated pyrazole moiety as anticancer and antimicrobial agents.合成及含吡唑杂环的查尔酮类衍生物的生物评价作为抗癌和抗菌剂。
Appl Biochem Biotechnol. 2012 Nov;168(5):1153-62. doi: 10.1007/s12010-012-9848-8. Epub 2012 Sep 5.
6
Synthesis and antimicrobial studies on novel chloro-fluorine containing hydroxy pyrazolines.新型含氯氟羟基吡唑啉的合成与抗菌研究
Eur J Med Chem. 2007 Jan;42(1):30-6. doi: 10.1016/j.ejmech.2006.07.011. Epub 2006 Sep 26.
7
Synthesis and biological evaluation of a novel series of pyrazole chalcones as anti-inflammatory, antioxidant and antimicrobial agents.新型吡唑查耳酮类化合物的合成及抗炎、抗氧化和抗菌活性评价。
Bioorg Med Chem. 2009 Dec 15;17(24):8168-73. doi: 10.1016/j.bmc.2009.10.035. Epub 2009 Oct 22.
8
Synthesis of 2-substituted-N-carboxymethyl-1,5-benzothiazepin-4-ones and -1,4-benzothiazin-3-ones and their evaluation as angiotensin converting enzyme inhibitors.2-取代-N-羧甲基-1,5-苯并硫氮杂䓬-4-酮和-1,4-苯并噻嗪-3-酮的合成及其作为血管紧张素转换酶抑制剂的评价。
Farmaco. 1995 Feb;50(2):107-12.
9
Synthesis of novel keto-ACE analogues as domain-selective angiotensin I-converting enzyme inhibitors.新型酮基-ACE类似物作为结构域选择性血管紧张素I转换酶抑制剂的合成
Bioorg Med Chem Lett. 2006 Sep 1;16(17):4612-5. doi: 10.1016/j.bmcl.2006.06.003. Epub 2006 Jun 19.
10
QIGLF, a novel angiotensin I-converting enzyme-inhibitory peptide from egg white protein.蛋清蛋白来源的新型血管紧张素转化酶抑制肽 QIGLF。
J Sci Food Agric. 2011 Mar 30;91(5):921-6. doi: 10.1002/jsfa.4266. Epub 2011 Jan 11.

引用本文的文献

1
Synthesis, Spectroscopic, Electronic and Molecular Docking Studies of Pyrazole Based Chalcones as Potential Anticancer Agents.基于吡唑的查尔酮作为潜在抗癌剂的合成、光谱、电子和分子对接研究
J Fluoresc. 2025 Aug 16. doi: 10.1007/s10895-025-04520-7.
2
The Application of the Pyrazole Structure in the Structural Modification of Natural Products.吡唑结构在天然产物结构修饰中的应用。
Mini Rev Med Chem. 2025;25(8):628-652. doi: 10.2174/0113895575359419241211092252.
3
Comprehensive Insight into Green Synthesis Approaches, Structural Activity Relationship, and Therapeutic Potential of Pyrazolic Chalcone Derivative.
对吡唑基查尔酮衍生物的绿色合成方法、构效关系及治疗潜力的全面洞察。
Mini Rev Med Chem. 2025;25(7):539-577. doi: 10.2174/0113895575327555241024111038.
4
Novel Erlotinib-Chalcone Hybrids Diminish Resistance in Head and Neck Cancer by Inducing Multiple Cell Death Mechanisms.新型厄洛替尼-查尔酮杂合体通过诱导多种细胞死亡机制减弱头颈部癌症的耐药性。
Int J Mol Sci. 2023 Feb 9;24(4):3456. doi: 10.3390/ijms24043456.
5
TfOH mediated intermolecular electrocyclization for the synthesis of pyrazolines and its application in alkaloid synthesis.三氟甲磺酸介导的分子间电环化反应合成吡唑啉及其在生物碱合成中的应用。
RSC Adv. 2018 Aug 24;8(53):30071-30075. doi: 10.1039/c8ra05702h.
6
Synthesis of new pyrazolone and pyrazole-based adamantyl chalcones and antimicrobial activity.新型吡唑啉酮和吡唑烷酮金刚烷查耳酮的合成及抗菌活性。
Biosci Rep. 2020 Sep 30;40(9). doi: 10.1042/BSR20201950.
7
Cytotoxic Effects of Newly Synthesized Heterocyclic Candidates Containing Nicotinonitrile and Pyrazole Moieties on Hepatocellular and Cervical Carcinomas.新型含烟酰胺腈和吡唑部分的杂环候选物对肝癌和宫颈癌的细胞毒性作用。
Molecules. 2019 May 22;24(10):1965. doi: 10.3390/molecules24101965.
8
Biological Evaluation and Molecular Dynamics Simulation of Chalcone Derivatives as Epidermal Growth Factor-Tyrosine Kinase Inhibitors.姜酮类衍生物作为表皮生长因子酪氨酸激酶抑制剂的生物学评价及分子动力学模拟。
Molecules. 2019 Mar 20;24(6):1092. doi: 10.3390/molecules24061092.
9
Current status of pyrazole and its biological activities.吡唑及其生物活性的当前状况。
J Pharm Bioallied Sci. 2016 Jan-Mar;8(1):2-17. doi: 10.4103/0975-7406.171694.
10
Antimicrobial screening and one-pot synthesis of 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives.4-(取代苯胺甲基)-3-(2-萘基)-1-苯基-1H-吡唑衍生物的抗菌筛选及一锅法合成
J Pharm Bioallied Sci. 2014 Oct;6(4):253-9. doi: 10.4103/0975-7406.142956.