• 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

新型茚满酮衍生物作为多功能抗阿尔茨海默病药物的设计、合成及方法

Design, Synthesis, and and Approaches of Novel Indanone Derivatives as Multifunctional Anti-Alzheimer Agents.

作者信息

Sağlık Begüm Nurpelin, Levent Serkan, Osmaniye Derya, Evren Asaf Evrim, Karaduman Abdullah Burak, Özkay Yusuf, Kaplancıklı Zafer Asım

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.

Central Research Laboratory (MERLAB), Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.

出版信息

ACS Omega. 2022 Dec 7;7(50):47378-47404. doi: 10.1021/acsomega.2c06906. eCollection 2022 Dec 20.

DOI:10.1021/acsomega.2c06906
PMID:36570177
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9774391/
Abstract

Alzheimer's disease (AD) is a neurological, progressive illness that typically affects the elderly and is clinically distinguished by memory and cognitive decline. Due to a number of factors, including the absence of a radical treatment, an increase in the patient population over time, the high cost of care and treatment, and a significant decline in patients' quality of life, the importance of this disease has increased. These factors have all prompted increased interest among researchers in this field. The chemical structure of the donepezil molecule, the most popular and effective treatment response for AD, served as the basis for the design and synthesis of 42 novel indan-1-one derivatives in this study. Using IR, H, and C NMR as well as mass spectroscopic techniques, the compounds' structures were identified. Research on the compounds' antioxidant activities, cholinesterase (ChE) enzyme inhibition, monoamine oxidase (MAO) A and B inhibitory activities, β-amyloid plaque inhibition, and cytotoxicity impact was carried out. Inhibition of β-amyloid plaque aggregation; effective inhibition of AChE, BChE, and MAO-B enzymes; and significant antioxidant activity were all demonstrated by compounds - and -. Because of their various actions, it was hypothesized that the related compounds may be useful in treating AD symptoms as well as providing palliative care.

摘要

阿尔茨海默病(AD)是一种神经退行性疾病,通常影响老年人,临床特征为记忆和认知能力下降。由于多种因素,包括缺乏根治性治疗方法、患者数量随时间增加、护理和治疗成本高昂以及患者生活质量显著下降,这种疾病的重要性日益凸显。这些因素促使该领域的研究人员对其兴趣大增。本研究中,多奈哌齐分子(AD最常用且有效的治疗药物)的化学结构成为设计和合成42种新型茚满-1-酮衍生物的基础。利用红外光谱(IR)、氢核磁共振(H NMR)、碳核磁共振(C NMR)以及质谱技术确定了这些化合物的结构。对这些化合物的抗氧化活性、胆碱酯酶(ChE)抑制作用、单胺氧化酶(MAO)A和B抑制活性、β-淀粉样蛋白斑块抑制作用以及细胞毒性影响进行了研究。化合物 - 和 - 均表现出抑制β-淀粉样蛋白斑块聚集、有效抑制乙酰胆碱酯酶(AChE)、丁酰胆碱酯酶(BChE)和单胺氧化酶B(MAO-B)以及显著的抗氧化活性。鉴于其多种作用,推测相关化合物可能有助于治疗AD症状并提供姑息治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/78669bb51377/ao2c06906_0022.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/ba52a2db31b9/ao2c06906_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/4b25d988fb4f/ao2c06906_0023.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/31cf17488b2a/ao2c06906_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/bd45f1644412/ao2c06906_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/b76ea0591bac/ao2c06906_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/61407e8ea4ae/ao2c06906_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/9cf9016cbf57/ao2c06906_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/789a15d35d0b/ao2c06906_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/741865dfefe0/ao2c06906_0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/1ebb31ef4773/ao2c06906_0009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/daf7a8f573a6/ao2c06906_0010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/668131dedc80/ao2c06906_0011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/4ab285c147a3/ao2c06906_0012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/e97bf5413ac6/ao2c06906_0013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/5ea97d7efddb/ao2c06906_0014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/529486156a39/ao2c06906_0015.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/c5dfa507e609/ao2c06906_0016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/7cdebb16d1e5/ao2c06906_0017.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/d4a17b3fac87/ao2c06906_0018.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/a8358e5febff/ao2c06906_0019.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/82e054020dd7/ao2c06906_0020.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/e3a7dc10a6b4/ao2c06906_0021.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/78669bb51377/ao2c06906_0022.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/ba52a2db31b9/ao2c06906_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/4b25d988fb4f/ao2c06906_0023.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/31cf17488b2a/ao2c06906_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/bd45f1644412/ao2c06906_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/b76ea0591bac/ao2c06906_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/61407e8ea4ae/ao2c06906_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/9cf9016cbf57/ao2c06906_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/789a15d35d0b/ao2c06906_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/741865dfefe0/ao2c06906_0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/1ebb31ef4773/ao2c06906_0009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/daf7a8f573a6/ao2c06906_0010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/668131dedc80/ao2c06906_0011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/4ab285c147a3/ao2c06906_0012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/e97bf5413ac6/ao2c06906_0013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/5ea97d7efddb/ao2c06906_0014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/529486156a39/ao2c06906_0015.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/c5dfa507e609/ao2c06906_0016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/7cdebb16d1e5/ao2c06906_0017.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/d4a17b3fac87/ao2c06906_0018.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/a8358e5febff/ao2c06906_0019.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/82e054020dd7/ao2c06906_0020.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/e3a7dc10a6b4/ao2c06906_0021.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ebb/9774391/78669bb51377/ao2c06906_0022.jpg

相似文献

1
Design, Synthesis, and and Approaches of Novel Indanone Derivatives as Multifunctional Anti-Alzheimer Agents.新型茚满酮衍生物作为多功能抗阿尔茨海默病药物的设计、合成及方法
ACS Omega. 2022 Dec 7;7(50):47378-47404. doi: 10.1021/acsomega.2c06906. eCollection 2022 Dec 20.
2
Investigation of Novel Benzoxazole-Oxadiazole Derivatives as Effective Anti-Alzheimer's Agents: In Vitro and In Silico Approaches.新型苯并恶唑-恶二唑衍生物作为有效抗阿尔茨海默病药物的研究:体外和计算机模拟方法
Pharmaceuticals (Basel). 2023 Jun 21;16(7):909. doi: 10.3390/ph16070909.
3
Design, synthesis, biological activity, molecular docking, and molecular dynamics of novel benzimidazole derivatives as potential AChE/MAO-B dual inhibitors.新型苯并咪唑衍生物作为潜在的 AChE/MAO-B 双重抑制剂的设计、合成、生物活性、分子对接和分子动力学研究。
Arch Pharm (Weinheim). 2022 Mar;355(3):e2100450. doi: 10.1002/ardp.202100450. Epub 2021 Dec 20.
4
Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.设计、合成、计算机模拟及新型查尔酮-O-氨基甲酸酯衍生物的生物学评价——作为治疗阿尔茨海默病的多功能药物。
Eur J Med Chem. 2019 Sep 15;178:726-739. doi: 10.1016/j.ejmech.2019.06.026. Epub 2019 Jun 14.
5
Synthesis and evaluation of 7-substituted coumarin derivatives as multimodal monoamine oxidase-B and cholinesterase inhibitors for the treatment of Alzheimer's disease.7-取代香豆素衍生物作为多模式单胺氧化酶-B和胆碱酯酶抑制剂用于治疗阿尔茨海默病的合成与评价
Eur J Med Chem. 2017 Jan 5;125:853-864. doi: 10.1016/j.ejmech.2016.09.041. Epub 2016 Sep 15.
6
Multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease: design, synthesis, biochemical evaluation, ADMET, molecular modeling, and QSAR analysis of novel donepezil-pyridyl hybrids.用于治疗阿尔茨海默病的多能胆碱酯酶/单胺氧化酶抑制剂:新型多奈哌齐 - 吡啶基杂化物的设计、合成、生化评价、ADMET、分子建模和QSAR分析
Drug Des Devel Ther. 2014 Oct 13;8:1893-910. doi: 10.2147/DDDT.S69258. eCollection 2014.
7
Synthesis of 4-substituted benzyl-2-triazole-linked-tryptamine-paeonol derivatives and evaluation of their selective inhibitions against butyrylcholinesterase and monoamine oxidase-B.合成 4-取代苄基-2-三唑连接色胺-丹皮酚衍生物,并评价它们对丁酰胆碱酯酶和单胺氧化酶-B 的选择性抑制作用。
Int J Biol Macromol. 2022 Sep 30;217:910-921. doi: 10.1016/j.ijbiomac.2022.07.178. Epub 2022 Jul 28.
8
Antioxidant and Cholinesterase Inhibitory Activities of Ethyl Acetate Extract of : Cell-free and Studies.[提取物名称]乙酸乙酯提取物的抗氧化及胆碱酯酶抑制活性:无细胞研究
Pharmacogn Mag. 2017 Oct;13(Suppl 3):S437-S445. doi: 10.4103/pm.pm_57_17. Epub 2017 Oct 11.
9
Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.新型多奈哌齐-吲哚基杂合物作为多效胆碱酯酶/单胺氧化酶抑制剂用于潜在治疗阿尔茨海默病的设计、合成、药理学评价、定量构效关系分析、分子模拟及药物代谢动力学/药物毒性预测
Eur J Med Chem. 2014 Mar 21;75:82-95. doi: 10.1016/j.ejmech.2013.12.028. Epub 2014 Jan 27.
10
N-alkylpiperidine carbamates as potential anti-Alzheimer's agents.N-烷基哌啶氨基甲酸酯类作为潜在的抗阿尔茨海默病药物。
Eur J Med Chem. 2020 Jul 1;197:112282. doi: 10.1016/j.ejmech.2020.112282. Epub 2020 Apr 15.

引用本文的文献

1
Novel Benzofuran-3-yl-methyl and Aliphatic Azacyclics: Design, Synthesis, and In Vitro and In Silico anti-Alzheimer Disease Activity Studies.新型苯并呋喃-3-基甲基和脂肪族氮杂环化合物:设计、合成以及体外和计算机模拟抗阿尔茨海默病活性研究
ACS Omega. 2025 Jul 22;10(30):32829-32843. doi: 10.1021/acsomega.5c01432. eCollection 2025 Aug 5.
2
Discovery of Novel Thiazolohydrazone Derivatives as an Alternative Option in the Treatment of Zoonotic Toxocara canis: In Vitro and In Silico Evaluation.新型噻唑腙衍生物作为治疗人兽共患犬弓首蛔虫替代方案的发现:体外和计算机模拟评估
Vet Med Sci. 2025 Jan;11(1):e70144. doi: 10.1002/vms3.70144.
3

本文引用的文献

1
Synthesis of novel benzothiazole derivatives and investigation of their enzyme inhibitory effects against Alzheimer's disease.新型苯并噻唑衍生物的合成及其对阿尔茨海默病的酶抑制作用研究
RSC Adv. 2022 Aug 19;12(36):23626-23636. doi: 10.1039/d2ra03803j. eCollection 2022 Aug 16.
2
Antidepressant-like effect of tofisopam in mice: A behavioural, molecular docking and MD simulation study.托吡酯样抗抑郁作用的研究:行为学、分子对接和 MD 模拟研究。
J Psychopharmacol. 2022 Jul;36(7):819-835. doi: 10.1177/02698811221095528. Epub 2022 May 30.
3
Design, Synthesis, and Evaluation of Novel 2-Benzo[b][1,4]thiazin-3(4)-one Derivatives as New Acetylcholinesterase Inhibitors.
Design, Synthesis, Investigation, and Biological Activity Assessments of (4-Substituted-Phenyl)--(3-morpholinopropyl)-3-phenylthiazol-2(3)-imine Derivatives as Antifungal Agents.
(4-取代苯基)-(3-吗啉基丙基)-3-苯基噻唑-2(3)-亚胺衍生物作为抗真菌剂的设计、合成、研究及生物活性评估
ACS Omega. 2024 Sep 16;9(38):39326-39343. doi: 10.1021/acsomega.3c07879. eCollection 2024 Sep 24.
4
Design, Synthesis, and Evaluation of New Pyrazolines As Small Molecule Inhibitors of Acetylcholinesterase.新型吡唑啉作为乙酰胆碱酯酶小分子抑制剂的设计、合成与评价
ACS Omega. 2024 Jul 13;9(29):31401-31409. doi: 10.1021/acsomega.3c10490. eCollection 2024 Jul 23.
5
NMR-Based Metabolomics to Analyze the Effects of a Series of Monoamine Oxidases-B Inhibitors on U251 Cells.基于 NMR 的代谢组学分析一系列单胺氧化酶-B 抑制剂对 U251 细胞的影响。
Biomolecules. 2023 Mar 27;13(4):600. doi: 10.3390/biom13040600.
新型 2-苯并[b][1,4]噻嗪-3(4H)-酮衍生物的设计、合成与乙酰胆碱酯酶抑制活性评价。
Molecules. 2022 Mar 25;27(7):2121. doi: 10.3390/molecules27072121.
4
Synthesis of novel thiazolyl hydrazone derivatives as potent dual monoamine oxidase-aromatase inhibitors.合成新型噻唑基腙衍生物作为有效的双重单胺氧化酶-芳香酶抑制剂。
Eur J Med Chem. 2022 Feb 5;229:114097. doi: 10.1016/j.ejmech.2021.114097. Epub 2022 Jan 1.
5
Design, synthesis, biological activity, molecular docking, and molecular dynamics of novel benzimidazole derivatives as potential AChE/MAO-B dual inhibitors.新型苯并咪唑衍生物作为潜在的 AChE/MAO-B 双重抑制剂的设计、合成、生物活性、分子对接和分子动力学研究。
Arch Pharm (Weinheim). 2022 Mar;355(3):e2100450. doi: 10.1002/ardp.202100450. Epub 2021 Dec 20.
6
Novel 2,5-disubstituted-1,3,4-oxadiazole derivatives as MAO-B inhibitors: Synthesis, biological evaluation and molecular modeling studies.新型 2,5-二取代-1,3,4-噁二唑衍生物作为 MAO-B 抑制剂的合成、生物评价及分子模拟研究。
Bioorg Chem. 2021 Jul;112:104917. doi: 10.1016/j.bioorg.2021.104917. Epub 2021 Apr 16.
7
Synthesis and biological evaluation of new pyrazolone Schiff bases as monoamine oxidase and cholinesterase inhibitors.新型吡唑酮席夫碱的合成及作为单胺氧化酶和胆碱酯酶抑制剂的生物评价。
Bioorg Chem. 2019 Mar;84:41-50. doi: 10.1016/j.bioorg.2018.11.016. Epub 2018 Nov 17.
8
Synthesis and Biological Evaluation of New Cholinesterase Inhibitors for Alzheimer's Disease.新型阿尔茨海默病乙酰胆碱酯酶抑制剂的合成与生物评价。
Molecules. 2018 Aug 14;23(8):2033. doi: 10.3390/molecules23082033.
9
Design, synthesis and biological assessment of new thiazolylhydrazine derivatives as selective and reversible hMAO-A inhibitors.新型噻唑基肼衍生物作为选择性和可逆性人单胺氧化酶-A抑制剂的设计、合成及生物学评价
Eur J Med Chem. 2018 Jan 20;144:68-81. doi: 10.1016/j.ejmech.2017.12.013. Epub 2017 Dec 6.
10
MAO enzymes inhibitory activity of new benzimidazole derivatives including hydrazone and propargyl side chains.含腙和炔丙基侧链的新型苯并咪唑衍生物的单胺氧化酶(MAO)酶抑制活性
Eur J Med Chem. 2017 May 5;131:92-106. doi: 10.1016/j.ejmech.2017.03.009. Epub 2017 Mar 8.