• 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

新型脒腙衍生酰肼作为潜在抗炎剂的合成与评价

Synthesis and evaluation of new amidrazone-derived hydrazides as a potential anti-inflammatory agents.

作者信息

Paprocka Renata, Wiese-Szadkowska Małgorzata, Helmin-Basa Anna, Mazur Liliana, Kutkowska Jolanta, Michałkiewicz Jacek, Modzelewska-Banachiewicz Bożena, Pazderski Leszek

机构信息

1Department of Organic Chemistry, Faculty of Pharmacy, Nicolaus Copernicus University in Toruń, Bydgoszcz, Poland.

2Department of Immunology, Faculty of Pharmacy, Nicolaus Copernicus University in Toruń, Bydgoszcz, Poland.

出版信息

Monatsh Chem. 2018;149(8):1493-1500. doi: 10.1007/s00706-018-2197-8. Epub 2018 Jun 27.

DOI:10.1007/s00706-018-2197-8
PMID:30100633
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6060958/
Abstract

ABSTRACT

The series of new hydrazide derivatives were synthesized in reactions of N-substituted amidrazones with cyclic anhydrides as potential anti-inflammatory and antibacterial agents. The compounds were characterized by H-C two-dimensional NMR techniques, which revealed the presence of two tautomeric forms in DMSO- solutions, while the molecular structure of one species was confirmed by single-crystal X-ray diffraction. The anti-inflammatory effects of hydrazides on peripheral blood mononuclear cells were experimentally evaluated. Three compounds showed antiproliferative activity comparable to ibuprofen. One derivative demonstrated strong reduction of lymphocyte proliferation stimulated by anti-CD3 antibody (by 90%) and PHA, as well as low cell toxicity. The obtained compounds exhibited relatively weak antibacterial activity; they were more effective against Gram-positive bacterial strains.

摘要

摘要

通过N-取代脒腙与环状酸酐反应合成了一系列新型酰肼衍生物，作为潜在的抗炎和抗菌剂。这些化合物通过H-C二维核磁共振技术进行了表征，结果表明在二甲基亚砜溶液中存在两种互变异构形式，同时通过单晶X射线衍射确定了其中一种异构体的分子结构。通过实验评估了酰肼对外周血单核细胞的抗炎作用。三种化合物表现出与布洛芬相当的抗增殖活性。一种衍生物对抗CD3抗体（降低90%）和植物血凝素刺激的淋巴细胞增殖有强烈抑制作用，且细胞毒性较低。所得到的化合物表现出相对较弱的抗菌活性；它们对革兰氏阳性细菌菌株更有效。

相似文献

1
Synthesis and evaluation of new amidrazone-derived hydrazides as a potential anti-inflammatory agents.新型脒腙衍生酰肼作为潜在抗炎剂的合成与评价
Monatsh Chem. 2018;149(8):1493-1500. doi: 10.1007/s00706-018-2197-8. Epub 2018 Jun 27.
2
Synthesis and Structural Study of Amidrazone Derived Pyrrole-2,5-Dione Derivatives: Potential Anti-Inflammatory Agents.酰胺腙衍生吡咯-2,5-二酮衍生物的合成及结构研究：潜在的抗炎剂。
Molecules. 2022 Apr 30;27(9):2891. doi: 10.3390/molecules27092891.
3
Synthesis, crystal structure and biological activities of a novel amidrazone derivative and its copper(II) complex--a potential antitumor drug.新型酰腙衍生物及其铜（II）配合物的合成、晶体结构和生物活性——一种潜在的抗肿瘤药物。
J Inorg Biochem. 2012 Sep;114:55-64. doi: 10.1016/j.jinorgbio.2012.04.021. Epub 2012 May 10.
4
A Review of the Biological Activity of Amidrazone Derivatives.脒腙衍生物的生物活性综述。
Pharmaceuticals (Basel). 2022 Sep 30;15(10):1219. doi: 10.3390/ph15101219.
5
Synthesis and anti-inflammatory activity of new 1,2,4-triazole derivatives.新型1,2,4-三唑衍生物的合成及抗炎活性
Bioorg Med Chem Lett. 2015 Jul 1;25(13):2664-7. doi: 10.1016/j.bmcl.2015.04.079. Epub 2015 Apr 30.
6
Evaluation of Anthelmintic and Anti-Inflammatory Activity of 1,2,4-Triazole Derivatives.评价 1,2,4-三唑衍生物的驱虫和抗炎活性。
Molecules. 2022 Jul 13;27(14):4488. doi: 10.3390/molecules27144488.
7
Synthesis and antibacterial evaluation of New N-acylhydrazone derivatives from dehydroabietic acid.从去氢枞酸中合成新型 N-酰腙衍生物及其抗菌评价。
Molecules. 2012 Apr 20;17(4):4634-50. doi: 10.3390/molecules17044634.
8
Reactions of N(3) -substituted amidrazones with cis-1,2-cyclohexanedicarboxylic anhydride and biological activities of the products.N(3) -取代的缩氨基脲与顺-1,2-环己烷二羧酸酐的反应及产物的生物活性。
Arch Pharm (Weinheim). 2012 Jun;345(6):486-94. doi: 10.1002/ardp.201100333. Epub 2012 Feb 3.
9
New Hydrazides and Hydrazide-Hydrazones of 2,3-Dihalogen Substituted Propionic Acids: Synthesis and in vitro Antimicrobial Activity Evaluation.2,3-二卤代丙酸的新型酰肼及酰肼腙：合成与体外抗菌活性评价
Chem Biodivers. 2017 Aug;14(8). doi: 10.1002/cbdv.201700075. Epub 2017 Jun 26.
10
Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety.评价含丙酸部分的新型 1,2,4-三唑衍生物的生物活性。
Molecules. 2023 Apr 29;28(9):3808. doi: 10.3390/molecules28093808.

引用本文的文献

1
Modeling of Effectiveness of -Substituted Amidrazone Derivatives as Potential Agents against Gram-Positive Bacteria.-取代的 amidrazone 衍生物作为抗革兰氏阳性菌潜在药物的效果建模。
Molecules. 2024 May 17;29(10):2369. doi: 10.3390/molecules29102369.
2
Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety.评价含丙酸部分的新型 1,2,4-三唑衍生物的生物活性。
Molecules. 2023 Apr 29;28(9):3808. doi: 10.3390/molecules28093808.
3
A Review of the Biological Activity of Amidrazone Derivatives.

本文引用的文献

1
ANTIBACTERIAL AND CENTRAL NERVOUS SYSTEM ACTIVITY OF (4,5-DIARYL-4H-1,2,4-TRIAZOL-3-YL)METHACRYLIC ACID DERIVATIVES.（4,5-二芳基-4H-1,2,4-三唑-3-基）甲基丙烯酸衍生物的抗菌及中枢神经系统活性
Acta Pol Pharm. 2017 Jan;74(1):289-292.
2
Global antibacterial resistance: The never-ending story.全球抗菌药物耐药性：永无休止的故事。
J Glob Antimicrob Resist. 2013 Jun;1(2):63-69. doi: 10.1016/j.jgar.2013.03.010. Epub 2013 Apr 30.
3
Synthesis and anti-inflammatory activity of new 1,2,4-triazole derivatives.新型1,2,4-三唑衍生物的合成及抗炎活性
脒腙衍生物的生物活性综述。
Pharmaceuticals (Basel). 2022 Sep 30;15(10):1219. doi: 10.3390/ph15101219.
4
Evaluation of Anthelmintic and Anti-Inflammatory Activity of 1,2,4-Triazole Derivatives.评价 1,2,4-三唑衍生物的驱虫和抗炎活性。
Molecules. 2022 Jul 13;27(14):4488. doi: 10.3390/molecules27144488.
5
Synthesis and Structural Study of Amidrazone Derived Pyrrole-2,5-Dione Derivatives: Potential Anti-Inflammatory Agents.酰胺腙衍生吡咯-2,5-二酮衍生物的合成及结构研究：潜在的抗炎剂。
Molecules. 2022 Apr 30;27(9):2891. doi: 10.3390/molecules27092891.
Bioorg Med Chem Lett. 2015 Jul 1;25(13):2664-7. doi: 10.1016/j.bmcl.2015.04.079. Epub 2015 Apr 30.
4
Antimicrobial activity of ibuprofen: new perspectives on an "Old" non-antibiotic drug.布洛芬的抗菌活性：一种“老”非抗生素药物的新视角。
Eur J Pharm Sci. 2015 Apr 25;71:93-8. doi: 10.1016/j.ejps.2015.02.011. Epub 2015 Feb 20.
5
Synthesis and biological activities of some new isonicotinic acid 2-(2-hydroxy-8-substituted-tricyclo[7.3.1.0(2.7)]tridec-13-ylidene)-hydrazides.某些新型异烟酸 2-(2-羟基-8-取代-三环[7.3.1.0(2.7)]十三碳-13-亚基)-酰肼的合成与生物活性
Bioorg Med Chem. 2015 Feb 1;23(3):401-10. doi: 10.1016/j.bmc.2014.12.038. Epub 2014 Dec 26.
6
Antibacterial activities of novel nicotinic acid hydrazides and their conversion into N-acetyl-1,3,4-oxadiazoles.新型烟酸酰肼的抗菌活性及其向N-乙酰基-1,3,4-恶二唑的转化
Bioorg Med Chem Lett. 2014 Dec 15;24(24):5796-5800. doi: 10.1016/j.bmcl.2014.10.029. Epub 2014 Oct 24.
7
Determination of preferred conformations of ibuprofen in chloroform by 2D NOE spectroscopy.通过二维核欧沃豪斯效应光谱法测定布洛芬在氯仿中的优势构象
Eur J Pharm Sci. 2014 Dec 18;65:65-73. doi: 10.1016/j.ejps.2014.08.005. Epub 2014 Sep 16.
8
Synthesis and antimicrobial activity of some novel hydrazide, benzochromenone, dihydropyridine, pyrrole, thiazole and thiophene derivatives.合成及某些新型酰肼、苯并色酮、二氢吡啶、吡咯、噻唑和噻吩衍生物的抗菌活性。
Eur J Med Chem. 2013;70:419-26. doi: 10.1016/j.ejmech.2013.09.003. Epub 2013 Oct 12.
9
TCH-1030 targeting on topoisomerase I induces S-phase arrest, DNA fragmentation, and cell death of breast cancer cells.TCH-1030 通过靶向拓扑异构酶 I 诱导乳腺癌细胞 S 期停滞、DNA 片段化和细胞死亡。
Breast Cancer Res Treat. 2013 Apr;138(2):383-93. doi: 10.1007/s10549-013-2441-1. Epub 2013 Feb 22.
10
Synthesis and anti-inflammatory activity of hydrazide derivatives of 2-methylidene-1,4-dicarboxybutanoic acid.
Acta Pol Pharm. 2012 Nov-Dec;69(6):1390-4.