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Future medicinal chemistry最新文献

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Semicarbazone, thiosemicarbazone tailed isoxazoline-pyrazole: synthesis, DFT, biological and computational assessment. 半咔唑酮、硫代咔唑酮尾部异噁唑啉-吡唑：合成、DFT、生物学和计算评估。
IF 4.2 4区 医学
Future medicinal chemistry Pub Date : 2024-09-18 DOI: 10.1080/17568919.2024.2394011
Abdoullah Bimoussa,Mouhi Eddine Hachim,Khalil El Khatabi,Yassine Laamari,Ali Oubella,Mohamed F AlAjmi,Aziz Auhmani,Mohammed Aziz Ajana,Hamid Morjani,My Youssef Ait Itto
{"title":"Semicarbazone, thiosemicarbazone tailed isoxazoline-pyrazole: synthesis, DFT, biological and computational assessment.","authors":"Abdoullah Bimoussa,Mouhi Eddine Hachim,Khalil El Khatabi,Yassine Laamari,Ali Oubella,Mohamed F AlAjmi,Aziz Auhmani,Mohammed Aziz Ajana,Hamid Morjani,My Youssef Ait Itto","doi":"10.1080/17568919.2024.2394011","DOIUrl":"https://doi.org/10.1080/17568919.2024.2394011","url":null,"abstract":"Aim: A series of semicarbazone and thiosemicarbazone-tailed hybrids comprising pyrazole and acetylisoxazoline were prepared from (R)-carvone and characterized by technique spectroscopies Nuclear Magnetic Resonance (NMR), IR and High-Resolution Mass Spectrometry. Density Functional Theory (DFT) determined the structural parameters. Their cytotoxic activity was evaluated in vitro against four human cancer cell lines.Methods & results: All the studied semi and thiosemicarbazone demonstrate a promising potential as anticancer agents. The mechanism of action of these compounds involves apoptosis in HT-1080 cells, supported by an increase in the level of caspase-3/7 activity, which also arrests the cell cycle in the G0/G1 phase. Molecular docking studies were performed to establish the potential of the most active compounds 4a and 5a. ADMET analysis showed appropriate pharmacokinetic properties, allowing structure prediction for anticancer activity.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":"9 1","pages":"1-14"},"PeriodicalIF":4.2,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142259951","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
One-pot synthesis and pharmacological evaluation of new quinoline/pyrimido-diazepines as pulmonary antifibrotic agents. 作为肺部抗纤维化药物的新型喹啉/嘧啶二氮杂卓的单锅合成和药理学评价。
IF 4.2 4区 医学
Future medicinal chemistry Pub Date : 2024-09-18 DOI: 10.1080/17568919.2024.2394018
Michael Atef Fawzy,Karim Hagag Ibrahim,Ashraf A Aly,Asmaa H Mohamed,Sara Mohamed Naguib Abdel Hafez,Walaa Yehia Abdelzaher,Eslam B Elkaeed,Aisha A Alsfouk,El-Shimaa Mn Abdelhafez
{"title":"One-pot synthesis and pharmacological evaluation of new quinoline/pyrimido-diazepines as pulmonary antifibrotic agents.","authors":"Michael Atef Fawzy,Karim Hagag Ibrahim,Ashraf A Aly,Asmaa H Mohamed,Sara Mohamed Naguib Abdel Hafez,Walaa Yehia Abdelzaher,Eslam B Elkaeed,Aisha A Alsfouk,El-Shimaa Mn Abdelhafez","doi":"10.1080/17568919.2024.2394018","DOIUrl":"https://doi.org/10.1080/17568919.2024.2394018","url":null,"abstract":"Aim: Pulmonary fibrosis is a life threating disease which requires an immediate treatment and due to the limited medications, this study focused on synthesizing a series of quinoline-based pyrimidodiazepines 4a-f as a novel antifibrotic hit.Materials & methods: The target compounds were synthesized via a one-pot reaction then investigated in a rat model of lung fibrosis induced by bleomycin (BLM).Results: Results revealed significant attenuation of the tested pro-inflammatory cytokines, fibrotic genes and apoptotic markers; however, Bcl-2 was upregulated, indicating a protective effect against fibrosis. Moreover, the molecular docking studies highlighted promising interactions between compounds 4b and 4c and specific amino acids within the protein pockets of caspase-3 (ARG341 and THR177), malondialdehyde (LYS195, LYS118 and ARG188) and TNF-α (SER99 and NME102).Conclusion: Compounds 4b and 4c emerge as promising candidates for further preclinical investigation as pulmonary antifibrotic agents.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":"48 1","pages":"1-20"},"PeriodicalIF":4.2,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142259999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, biological and computational evaluation of benzoxazole hybrid analogs as potential anti-Alzheimer's agents. 苯并恶唑杂化类似物的合成、生物学和计算评估，作为潜在的抗阿尔茨海默氏症药物。
IF 4.2 4区 医学
Future medicinal chemistry Pub Date : 2024-09-13 DOI: 10.1080/17568919.2024.2393569
Mohamed S Othman,Rafaqat Hussain,Fazal Rahim,Hayat Ullah,Shoaib Khan,Muhammad Taha,Mohamed A Fareid,Anas T Altaleb,Shimaa M Aboelnaga,Syed Adnan Ali Shah
{"title":"Synthesis, biological and computational evaluation of benzoxazole hybrid analogs as potential anti-Alzheimer's agents.","authors":"Mohamed S Othman,Rafaqat Hussain,Fazal Rahim,Hayat Ullah,Shoaib Khan,Muhammad Taha,Mohamed A Fareid,Anas T Altaleb,Shimaa M Aboelnaga,Syed Adnan Ali Shah","doi":"10.1080/17568919.2024.2393569","DOIUrl":"https://doi.org/10.1080/17568919.2024.2393569","url":null,"abstract":"Aim: Current study aims exploration of bis-benzoxazole bearing bis-Schiff base scaffolds (1-16) as anti-Alzheimer's agents.Materials & methods: 2-aminophenol is used as starting materials which react with different reagents in different step to give us bis-benzoxazole bearing bis-Schiff base analogs. NMR and HREI-MS techniques were used for characterization. All derivatives demonstrated varied range of activities with IC50 values 1.10 ± 0.40-24.50 ± 0.90 μM against acetylcholinesterase (AChE) and 1.90 ± 0.70-28.60 ± 0.60 μM against butyrylcholinesterase (BuChE) in contrast to donepezil. In both cases, analog-3 was found most potent. Molecular docking explored modes of interactions between scaffolds and receptor sites of targeted enzymes.Conclusion: This study offering promising approach for optimization and development of potent inhibitors of cholinesterase enzymes.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":"25 1","pages":"1-11"},"PeriodicalIF":4.2,"publicationDate":"2024-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142259952","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A novel class of potent antiangiogenic and antioxidant pyrazoles: synthesis, bioactivity, docking and ADMET studies. 一类新型强效抗血管生成和抗氧化吡唑：合成、生物活性、对接和 ADMET 研究。
IF 4.2 4区 医学
Future medicinal chemistry Pub Date : 2024-09-12 DOI: 10.1080/17568919.2024.2394020
Siddaram Nadigar,Rohith Gattu,Sanjay Ramesh,Rekha N Dharmappa,Vijendra Kumar Nanjundaswamy,Suhas Ramesh
{"title":"A novel class of potent antiangiogenic and antioxidant pyrazoles: synthesis, bioactivity, docking and ADMET studies.","authors":"Siddaram Nadigar,Rohith Gattu,Sanjay Ramesh,Rekha N Dharmappa,Vijendra Kumar Nanjundaswamy,Suhas Ramesh","doi":"10.1080/17568919.2024.2394020","DOIUrl":"https://doi.org/10.1080/17568919.2024.2394020","url":null,"abstract":"Aim: Angiogenesis is the hallmark of cancer progression driven by VEGF/VEGFR-2 signalling pathway, inhibition of which could be a solution to tackle the progression of tumour cells and thus arresting their growth.Materials & methods: A novel class of pyrazoles was synthesized using arginine and dibromo ketones. Antiangiogenic activity was performed by in vivo yolk sac method. Antioxidant activity was evaluated by hydroxyl and superoxide radical scavenging assays. Docking studies were performed to determine the pyrazoles' binding potential with VEGFR-2 receptor and VEGF tyrosine kinase. ADMET properties were calculated using SwissADME and admetSAR for drug-likeness.Results: Compounds 5a-e showed significant antiangiogenic effects. Compound 5f exhibited effective hydroxyl and superoxide radical scavenging activities. Docking results confirmed the potential binding efficiency with VEGFR-2 receptor over VEGF tyrosine kinase, thus, functioning as competitive-inhibitors. ADMET studies revealed that the compounds possess favourable drug-like qualities.Conclusion: This study presents a novel class of pyrazoles as promising antioxidant and antiangiogenic agents with favourable drug-likeness properties.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":"88 1","pages":"1-16"},"PeriodicalIF":4.2,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142195506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of novel dihydro-pyrimidine hybrids: insight into the design, synthesis, biological evaluation and absorption, distribution, metabolism and excretion studies. 发现新型二氢嘧啶混合物：深入了解设计、合成、生物评估以及吸收、分布、代谢和排泄研究。
IF 4.2 4区 医学
Future medicinal chemistry Pub Date : 2024-09-12 DOI: 10.1080/17568919.2024.2389767
Uzma Arshad,Nusrat Shafiq,Shagufta Parveen,Maryam Rashid
{"title":"Discovery of novel dihydro-pyrimidine hybrids: insight into the design, synthesis, biological evaluation and absorption, distribution, metabolism and excretion studies.","authors":"Uzma Arshad,Nusrat Shafiq,Shagufta Parveen,Maryam Rashid","doi":"10.1080/17568919.2024.2389767","DOIUrl":"https://doi.org/10.1080/17568919.2024.2389767","url":null,"abstract":"Aim: By keeping in aspects, the pharmacological potential of heterocyclic compounds, pyrimidine-based compounds were designed, synthesized and evaluated for α-amylase inhibitory potential.Materials & methods: Five new series 1a-l, 2a-d, 3a-d, 4a-d and 5a-d of 1,2,3,4-tetrahydroprimidine-5-carboxylate derivatives were designed by de novo method by taking Alogliptin as reference compound. Here in we describe synthesis and characterization of compounds as potential α-amylase inhibitor.Results: Structure activity relationship (SAR), in vitro analysis and molecular modelling approaches generate compounds 1 h, 1i, 1k and 4c as potential lead with good α-amylase inhibitory selection. However, compound 1k failed the criteria of optimization as drug lead by ADME studies while all other compounds showed optimum range for all in silico ADME parameters.Conclusion: Therefore, these compounds can serve as potential lead candidate in developing anti-diabetic therapy.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":"16 1","pages":"1-21"},"PeriodicalIF":4.2,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142195505","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, anticancer activity, docking and computational studies of new pyridyl-glycosyl hybrids and acyclic analogs. 新型吡啶基-糖基杂交化合物和无环类似物的合成、抗癌活性、对接和计算研究。
IF 4.2 4区 医学
Future medicinal chemistry Pub Date : 2024-09-12 DOI: 10.1080/17568919.2024.2389768
Mohamed N El-Bayaa,Eman R Kotb,Sabri Messaoudi,Hanem M Awad,Mahmoud G Saleh,Hanan A Soliman
{"title":"Synthesis, anticancer activity, docking and computational studies of new pyridyl-glycosyl hybrids and acyclic analogs.","authors":"Mohamed N El-Bayaa,Eman R Kotb,Sabri Messaoudi,Hanem M Awad,Mahmoud G Saleh,Hanan A Soliman","doi":"10.1080/17568919.2024.2389768","DOIUrl":"https://doi.org/10.1080/17568919.2024.2389768","url":null,"abstract":"New pyridine-O-glycosides and their acyclic nucleoside analogues were prepared by heterocyclization and glycosylation. The anticancer activity against HCT-116, HepG2 and MCF-7 human cancer cells and BJ-1 cell revealed that the galacto- and xylopyranosyl glycosides possessing 4-bromophenyl have superior cytotoxic activities against HepG2 cell while glycosides 7-9 resulted in superior cytotoxic activities regarding MCF-7 breast cell. In case of HCT-116 colorectal carcinoma cells, two products and the derived glycosides and acyclic analogues showed potent activities. The most potent compounds were investigated for their possible binding affinities to the active site of CDK2 enzyme via in silico molecular docking simulation in addition to computational studies. The results support the antiproliferative effect and elucidate the interactions of 3a and 8 with catalytic sites.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":"167 1","pages":"1-15"},"PeriodicalIF":4.2,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142195504","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Protein-protein interactions in cGAS-STING pathway: a medicinal chemistry perspective. cGAS-STING 通路中蛋白质与蛋白质之间的相互作用：药物化学的视角。
IF 4.2 4区 医学
Future medicinal chemistry Pub Date : 2024-09-12 DOI: 10.1080/17568919.2024.2383164
Shi-Duo Zhang,Hui Li,Ye-Ling Zhou,Xue-Chun Liu,De-Chang Li,Chuan-Feng Hao,Qi-Dong You,Xiao-Li Xu
{"title":"Protein-protein interactions in cGAS-STING pathway: a medicinal chemistry perspective.","authors":"Shi-Duo Zhang,Hui Li,Ye-Ling Zhou,Xue-Chun Liu,De-Chang Li,Chuan-Feng Hao,Qi-Dong You,Xiao-Li Xu","doi":"10.1080/17568919.2024.2383164","DOIUrl":"https://doi.org/10.1080/17568919.2024.2383164","url":null,"abstract":"Protein-protein interactions (PPIs) play pivotal roles in biological processes and are closely linked with human diseases. Research on small molecule inhibitors targeting PPIs provides valuable insights and guidance for novel drug development. The cGAS-STING pathway plays a crucial role in regulating human innate immunity and is implicated in various pathological conditions. Therefore, modulators of the cGAS-STING pathway have garnered extensive attention. Given that this pathway involves multiple PPIs, modulating PPIs associated with the cGAS-STING pathway has emerged as a promising strategy for modulating this pathway. In this review, we summarize an overview of recent advancements in medicinal chemistry insights into cGAS-STING PPI-based modulators and propose alternative strategies for further drug discovery based on the cGAS-STING pathway.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":"40 1","pages":"1-20"},"PeriodicalIF":4.2,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142195507","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, crystal structure, biological and docking studies of 5-hydroxy-2-{[(2-methylpropyl)iminio]methyl}phenolate. 5-hydroxy-2-{[(2-methylpropyl)iminio]methyl}phenolate 的合成、晶体结构、生物学和对接研究。
IF 4.2 4区 医学
Future medicinal chemistry Pub Date : 2024-09-11 DOI: 10.1080/17568919.2024.2389763
Arjunan Ayyappan,Sebastian Arockiasamy
{"title":"Synthesis, crystal structure, biological and docking studies of 5-hydroxy-2-{[(2-methylpropyl)iminio]methyl}phenolate.","authors":"Arjunan Ayyappan,Sebastian Arockiasamy","doi":"10.1080/17568919.2024.2389763","DOIUrl":"https://doi.org/10.1080/17568919.2024.2389763","url":null,"abstract":"Background: Schiff base compounds are potential drugs.Results: A Schiff base compound prepared by condensing 2,4-dihydroxy benzaldehyde and isobutylamine was characterized for structure, thermal, physicochemical and biological properties. The keto-enol tautomerism and azomethine functionality enhances electron delocaliZation and biological activity. The compound showed good antibacterial and antifungal activity at 40 μg/ml against bacteria such as Escherichia coli and Staphylococcus aureus and fungi like Candida albicans and Candida tropicalis. The docking study exhibits a moderate binding affinity for the GyrB protein in E. coli with a binding energy of -4.26 kcal/mol.Conclusion: The compound exhibits enhanced biological activity and suppression of cell growth at concentrations as low as 30 μg/ml. The IC50 for MFC-7 was found to be 41.5 μg/ml.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":"42 1","pages":"1-16"},"PeriodicalIF":4.2,"publicationDate":"2024-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142195508","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
New pyridopyrimidine derivatives as dual EGFR and CDK4/cyclin D1 inhibitors: synthesis, biological screening and molecular modeling. 作为表皮生长因子受体和 CDK4/ 环素 D1 双重抑制剂的新型吡啶嘧啶衍生物：合成、生物筛选和分子建模。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-17 Epub Date: 2024-07-18 DOI: 10.1080/17568919.2024.2366147
Fatma Ma Krakisha, Dina Ia Othman, Walaa M El Husseiny, Magda Na Nasr
{"title":"New pyridopyrimidine derivatives as dual EGFR and CDK4/cyclin D1 inhibitors: synthesis, biological screening and molecular modeling.","authors":"Fatma Ma Krakisha, Dina Ia Othman, Walaa M El Husseiny, Magda Na Nasr","doi":"10.1080/17568919.2024.2366147","DOIUrl":"10.1080/17568919.2024.2366147","url":null,"abstract":"<p><p><b>Aim:</b> A series of pyridopyrimidine derivatives <b>5-20</b> was designed, synthesized and examined for antitumor activity using four types of malignant cells.<b>Materials & methods:</b> Cervical cancer (HeLa), hepatic cancer (HepG-2), breast cancer (MCF-7) and colon cancer (HCT-166) cells, as well as normal human lung fibroblast cells (WI-38) were used to determine the cytotoxicity.<b>Results:</b> Pyrazol-1-<i>yl</i> pyridopyrimidine derivative <b>5</b> was found to be the most active compound against three malignant cells Hela, MCF-7 and HepG-2 with IC<sub>50</sub> values of 9.27, 7.69 and 5.91 μM, respectively, related to standard Doxorubicin. Moreover, compounds <b>5</b> and <b>10</b> showed good inhibition against cyclin dependent kinase (CDK4/cyclin D1) and epidermal growth factor (EGFR) enzymes.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1633-1648"},"PeriodicalIF":3.2,"publicationDate":"2024-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370904/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141633145","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, characterization and biological evaluation of aurones as potential neuroprotective agents. 作为潜在神经保护剂的醛酮的合成、表征和生物学评估。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-17 Epub Date: 2024-06-28 DOI: 10.1080/17568919.2024.2363713
Muhammad Ayaz, Syed Wadood Ali Shah, Mohammad Shoaib, Fawad Ali Shah, Fawad Ahmed
{"title":"Synthesis, characterization and biological evaluation of aurones as potential neuroprotective agents.","authors":"Muhammad Ayaz, Syed Wadood Ali Shah, Mohammad Shoaib, Fawad Ali Shah, Fawad Ahmed","doi":"10.1080/17568919.2024.2363713","DOIUrl":"10.1080/17568919.2024.2363713","url":null,"abstract":"<p><p><b>Aim:</b> To synthesize aurone (Ar) derivatives and to demonstrate their effects against diabetes mellitus (DM) and neurodegeneration.<b>Materials & methods:</b> Five Ar (<b>A-E</b>) derivatives were synthesized, characterized by proton NMR and screened for antioxidant, anti-diabetic and anti-cholinesterase activities. They were further evaluated for neuroprotective effects in streptozotocin (STZ)-induced neurodegenerative model.<b>Results:</b> Among the aurone derivatives ArE demonstrated significant reversal of cognitive impairment, oxidative stress and neuroinflammation. Biochemical analysis revealed anti-diabetic and neuroprotective effects, possibly through downregulation of inflammatory markers and upregulation of antioxidant enzymes.<b>Conclusion:</b> Synthesized Ar (<b>A-E</b>) exhibits promising therapeutic potential against STZ-induced neurodegeneration and DM by modulating inflammatory and oxidative pathways, suggesting a novel avenue for disease management.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1649-1663"},"PeriodicalIF":3.2,"publicationDate":"2024-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370930/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141467407","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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