• 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

2-取代-4,6-二芳基嘧啶类化合物的合成、生物评价及分子对接研究作为α-葡萄糖苷酶抑制剂。

Synthesis, Biological Evaluation and Molecular Docking Study of 2-Substituted-4,6-Diarylpyrimidines as α-Glucosidase Inhibitors.

机构信息

Provincial Key Laboratory of Pharmaceutics in Guizhou Province, Guizhou Medical University, Beijing Road, Guiyang 550004, China.

School of Pharmacy, Guizhou Medical University, 4 Beijing Road, Guiyang 550004, China.

出版信息

Molecules. 2017 Oct 30;22(11):1865. doi: 10.3390/molecules22111865.

DOI:10.3390/molecules22111865
PMID:29084182
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6150375/
Abstract

A novel series of 2-substituted-4,6-diarylpyrimidines - has been synthesized, characterized by ¹H-NMR, C-NMR and HRMS, and screened for in vitro -glucosidase inhibitory activity. The majority of the screened compounds possessed significant α-glucosidase inhibitory activity with IC values ranging from 19.6 ± 0.21 to 38.9 ± 0.35 μM, which is more potent than the positive control α-glucosidase inhibitor acarbose (IC = 817.38 ± 6.27 μM). Among them, was found to be the most active compound against α-glucosidase with an IC of 19.6 ± 0.21 μM. In addition, molecular docking studies were carried out to explore the binding interactions of 2-substituted-4,6-diarylpyrimidine derivatives with α-glucosidase.

摘要

我们合成了一系列新型的 2-取代-4,6-二芳基嘧啶，并通过 ¹H-NMR、C-NMR 和高分辨率质谱（HRMS）对其进行了表征，同时对其体外α-葡萄糖苷酶抑制活性进行了筛选。大多数筛选出的化合物对α-葡萄糖苷酶具有显著的抑制活性，IC 值范围为 19.6 ± 0.21 至 38.9 ± 0.35 μM，其活性强于阳性对照 α-葡萄糖苷酶抑制剂阿卡波糖（IC = 817.38 ± 6.27 μM）。其中，化合物 表现出对 α-葡萄糖苷酶最强的抑制活性，IC 值为 19.6 ± 0.21 μM。此外，还进行了分子对接研究，以探索 2-取代-4,6-二芳基嘧啶衍生物与 α-葡萄糖苷酶的结合相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5973/6150375/d3296aee0ba5/molecules-22-01865-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5973/6150375/ef913ac1f332/molecules-22-01865-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5973/6150375/db8f4821f138/molecules-22-01865-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5973/6150375/3e57c7747a33/molecules-22-01865-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5973/6150375/d3296aee0ba5/molecules-22-01865-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5973/6150375/ef913ac1f332/molecules-22-01865-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5973/6150375/db8f4821f138/molecules-22-01865-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5973/6150375/3e57c7747a33/molecules-22-01865-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5973/6150375/d3296aee0ba5/molecules-22-01865-g003.jpg

相似文献

1
Synthesis, Biological Evaluation and Molecular Docking Study of 2-Substituted-4,6-Diarylpyrimidines as α-Glucosidase Inhibitors.2-取代-4,6-二芳基嘧啶类化合物的合成、生物评价及分子对接研究作为α-葡萄糖苷酶抑制剂。
Molecules. 2017 Oct 30;22(11):1865. doi: 10.3390/molecules22111865.
2
Synthesis, in vitro α-glucosidase inhibitory activity and docking studies of novel chromone-isatin derivatives.新型色酮-异吲哚酮衍生物的合成、体外α-葡萄糖苷酶抑制活性及对接研究
Bioorg Med Chem Lett. 2018 Jan 15;28(2):113-116. doi: 10.1016/j.bmcl.2017.11.047. Epub 2017 Nov 28.
3
Inhibitory activity evaluation and mechanistic studies of tetracyclic oxindole derivatives as α-glucosidase inhibitors.四环氧化吲哚衍生物作为α-葡萄糖苷酶抑制剂的抑制活性评估及作用机制研究
Eur J Med Chem. 2016 Nov 10;123:365-378. doi: 10.1016/j.ejmech.2016.07.044. Epub 2016 Jul 25.
4
Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as α-Glucosidase Inhibitors.新型异吲哚酮-噻唑衍生物作为α-葡萄糖苷酶抑制剂的合成、生物学评价及分子对接研究
Molecules. 2017 Apr 20;22(4):659. doi: 10.3390/molecules22040659.
5
Synthesis, in vitro evaluation and molecular docking studies of novel coumarin-isatin derivatives as α-glucosidase inhibitors.新型香豆素-异吲哚酮衍生物作为α-葡萄糖苷酶抑制剂的合成、体外评价及分子对接研究
Chem Biol Drug Des. 2017 Mar;89(3):456-463. doi: 10.1111/cbdd.12867. Epub 2016 Oct 5.
6
Synthesis, In Vitro α-Glucosidase Inhibitory Activity and Molecular Docking Studies of Novel Benzothiazole-Triazole Derivatives.新型苯并噻唑-三唑衍生物的合成、体外α-葡萄糖苷酶抑制活性及分子对接研究。
Molecules. 2017 Sep 15;22(9):1555. doi: 10.3390/molecules22091555.
7
Synthesis, biological evaluation, and docking studies of novel 5,6-diaryl-1,2,4-triazine thiazole derivatives as a new class of α-glucosidase inhibitors.新型 5,6-二芳基-1,2,4-三嗪噻唑衍生物的合成、生物评价及对接研究作为一类新型的α-葡萄糖苷酶抑制剂。
Bioorg Chem. 2018 Aug;78:195-200. doi: 10.1016/j.bioorg.2018.03.015. Epub 2018 Mar 21.
8
Synthesis, in vitro evaluation and molecular docking studies of novel triazine-triazole derivatives as potential α-glucosidase inhibitors.新型三嗪 - 三唑衍生物作为潜在α - 葡萄糖苷酶抑制剂的合成、体外评价及分子对接研究
Eur J Med Chem. 2017 Jan 5;125:423-429. doi: 10.1016/j.ejmech.2016.09.067. Epub 2016 Sep 21.
9
Synthesis and molecular docking studies of potent α-glucosidase inhibitors based on biscoumarin skeleton.基于双香豆素骨架的高效α-葡萄糖苷酶抑制剂的合成与分子对接研究
Eur J Med Chem. 2014 Jun 23;81:245-52. doi: 10.1016/j.ejmech.2014.05.010. Epub 2014 May 4.
10
Design, synthesis and biological evaluation of novel coumarin thiazole derivatives as α-glucosidase inhibitors.新型香豆素噻唑衍生物作为α-葡萄糖苷酶抑制剂的设计、合成及生物学评价
Bioorg Chem. 2016 Apr;65:167-74. doi: 10.1016/j.bioorg.2016.03.001. Epub 2016 Mar 2.

引用本文的文献

1
Chiral pyrimidinyl-piperazine carboxamide derivatives as potent yeast α-glucosidase inhibitors.手性嘧啶基哌嗪甲酰胺衍生物作为有效的酵母α-葡萄糖苷酶抑制剂
Sci Rep. 2025 Jul 2;15(1):23241. doi: 10.1038/s41598-025-06104-8.
2
Experimental and theoretical studies on structural changes in the microtubule affinity-regulating kinase 4 (MARK4) protein induced by -hetarenes: a new class of therapeutic candidates for Alzheimer's disease.关于杂芳烃诱导微管亲和调节激酶4（MARK4）蛋白结构变化的实验和理论研究：一类新的阿尔茨海默病治疗候选药物
Front Med (Lausanne). 2025 Mar 19;12:1529845. doi: 10.3389/fmed.2025.1529845. eCollection 2025.
3

本文引用的文献

1
Discovery of 3,3-di(indolyl)indolin-2-one as a novel scaffold for α-glucosidase inhibitors: In silico studies and SAR predictions.发现3,3-二（吲哚基）吲哚啉-2-酮作为α-葡萄糖苷酶抑制剂的新型骨架：计算机模拟研究和构效关系预测。
Bioorg Chem. 2017 Jun;72:228-233. doi: 10.1016/j.bioorg.2017.05.006. Epub 2017 May 3.
2
Synthesis of novel spiro[pyrazolo[4,3-d]pyrimidinones and spiro[benzo[4,5]thieno[2,3-d]pyrimidine-2,3'-indoline]-2',4(3H)-diones and their evaluation for anticancer activity.新型螺[吡唑并[4,3 - d]嘧啶酮]和螺[苯并[4,5]噻吩并[2,3 - d]嘧啶 - 2,3'-吲哚啉]-2',4(3H)-二酮的合成及其抗癌活性评价
Bioorg Med Chem Lett. 2017 Mar 15;27(6):1446-1450. doi: 10.1016/j.bmcl.2017.01.088. Epub 2017 Feb 1.
3
4,6-Disubstituted pyrimidine-based microtubule affinity-regulating kinase 4 (MARK4) inhibitors: synthesis, characterization, activity and studies.
基于4,6-二取代嘧啶的微管亲和调节激酶4（MARK4）抑制剂：合成、表征、活性及研究
Front Pharmacol. 2025 Jan 20;15:1517504. doi: 10.3389/fphar.2024.1517504. eCollection 2024.
4
A Review on the Development of Novel Heterocycles as α-Glucosidase Inhibitors for the Treatment of Type-2 Diabetes Mellitus.新型杂环类 α-葡萄糖苷酶抑制剂用于治疗 2 型糖尿病的研究进展综述。
Med Chem. 2024;20(5):503-536. doi: 10.2174/0115734064264591231031065639.
5
Discovery of Amide-Functionalized Benzimidazolium Salts as Potent α-Glucosidase Inhibitors.酰胺功能化苯并咪唑鎓盐作为有效的α-葡萄糖苷酶抑制剂的发现。
Molecules. 2021 Aug 6;26(16):4760. doi: 10.3390/molecules26164760.
6
Design, synthesis, molecular docking, and in vitro α-glucosidase inhibitory activities of novel 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines against yeast and rat α-glucosidase.新型 3-氨基-2,4-二芳基苯并[4,5]咪唑并[1,2-a]嘧啶对酵母和大鼠 α-葡萄糖苷酶的设计、合成、分子对接及体外抑制活性研究。
Sci Rep. 2021 Jun 7;11(1):11911. doi: 10.1038/s41598-021-91473-z.
7
Identification of hub genes related to the progression of type 1 diabetes by computational analysis.通过计算分析鉴定与 1 型糖尿病进展相关的枢纽基因。
BMC Endocr Disord. 2021 Apr 7;21(1):61. doi: 10.1186/s12902-021-00709-6.
8
Synthesis and characterisation of thiobarbituric acid enamine derivatives, and evaluation of their α-glucosidase inhibitory and anti-glycation activity.硫代巴比妥酸烯胺衍生物的合成与表征及其α-葡萄糖苷酶抑制和抗糖化活性评价。
J Enzyme Inhib Med Chem. 2020 Dec;35(1):692-701. doi: 10.1080/14756366.2020.1737045.
Design, synthesis and evaluation of novel pyrazolo-pyrimido[4,5-d]pyrimidine derivatives as potent antibacterial and biofilm inhibitors.
新型吡唑并嘧啶并[4,5-d]嘧啶衍生物作为强效抗菌和生物膜抑制剂的设计、合成与评价
Bioorg Med Chem Lett. 2017 Mar 15;27(6):1451-1457. doi: 10.1016/j.bmcl.2017.01.087. Epub 2017 Feb 3.
4
Synthesis, in vitro evaluation and molecular docking studies of novel triazine-triazole derivatives as potential α-glucosidase inhibitors.新型三嗪 - 三唑衍生物作为潜在α - 葡萄糖苷酶抑制剂的合成、体外评价及分子对接研究
Eur J Med Chem. 2017 Jan 5;125:423-429. doi: 10.1016/j.ejmech.2016.09.067. Epub 2016 Sep 21.
5
Synthesis, biological evaluation and molecular docking study of N-arylbenzo[d]oxazol-2-amines as potential α-glucosidase inhibitors.N-芳基苯并[d]恶唑-2-胺作为潜在α-葡萄糖苷酶抑制剂的合成、生物学评价及分子对接研究
Bioorg Med Chem. 2016 Nov 1;24(21):5374-5379. doi: 10.1016/j.bmc.2016.08.061. Epub 2016 Aug 30.
6
Synthesis of pyrazolo[1,5-a]pyrimidine derivatives and their antifungal activities against phytopathogenic fungi in vitro.吡唑并[1,5-a]嘧啶衍生物的合成及其对植物病原真菌的体外抗真菌活性。
Mol Divers. 2016 Nov;20(4):887-896. doi: 10.1007/s11030-016-9690-y. Epub 2016 Sep 7.
7
Synthesis of pyrimidine-2,4,6-trione derivatives: Anti-oxidant, anti-cancer, α-glucosidase, β-glucuronidase inhibition and their molecular docking studies.嘧啶-2,4,6-三酮衍生物的合成：抗氧化、抗癌、α-葡萄糖苷酶、β-葡萄糖醛酸酶抑制作用及其分子对接研究。
Bioorg Chem. 2016 Oct;68:72-9. doi: 10.1016/j.bioorg.2016.07.009. Epub 2016 Jul 19.
8
Ionic liquid-promoted multicomponent synthesis of fused tetrazolo[1,5-a]pyrimidines as α-glucosidase inhibitors.离子液体促进的稠合四唑并[1,5-a]嘧啶作为α-葡萄糖苷酶抑制剂的多组分合成。
Bioorg Med Chem Lett. 2016 Aug 15;26(16):4007-14. doi: 10.1016/j.bmcl.2016.06.086. Epub 2016 Jun 30.
9
Synthesis, in vitro biological activities and in silico study of dihydropyrimidines derivatives.二氢嘧啶衍生物的合成、体外生物活性及计算机模拟研究
Bioorg Med Chem. 2015 Oct 15;23(20):6740-8. doi: 10.1016/j.bmc.2015.09.001. Epub 2015 Sep 3.
10
Therapeutic potential of α-glucosidase inhibitors in type 2 diabetes mellitus: an evidence-based review.α-葡萄糖苷酶抑制剂在2型糖尿病中的治疗潜力：一项基于证据的综述。
Expert Opin Pharmacother. 2015;16(13):1959-81. doi: 10.1517/14656566.2015.1070827.