European Journal of Medicinal Chemistry Reports最新文献

{"title":"Engineered bacterial cellulose-based Ag nanoparticles/g-C3N4/Eucalyptus extract nanocomposites for wound dressing: In vitro evaluation","authors":"Maral Sorourian ,&nbsp;Mehrab Pourmadadi ,&nbsp;Fatemeh Yazdian ,&nbsp;Hamid Rashedi ,&nbsp;Mona Navaei Nigjeh ,&nbsp;Ghazal Sorourian ,&nbsp;Abbas Rahdar ,&nbsp;Sadanand Pandey","doi":"10.1016/j.ejmcr.2024.100190","DOIUrl":"10.1016/j.ejmcr.2024.100190","url":null,"abstract":"<div><p>In recent years, antibacterial wound dressings have gained considerable attention. Bacterial cellulose (BC) has received significant interest due to its unique physiochemical characteristics such as biocompatibility, high porosity, superior mechanical properties, water holding capacity, and nontoxicity. In this work, silver nanoparticles/graphitic carbon nitride/eucalyptus extract (Ag/gCN/EE) nanocomposite was synthesized as an antibacterial agent and incorporated into nanofibrous structures composed of BC. The BC/Ag/gCN/EE and polyvinyl alcohol/BC/Ag/gCN/EE (PVA/BC/Ag/gCN/EE) nanocomposites were synthesized using immersion and electrospinning methods, respectively. Then, the swelling ratio was optimized and the wound dressings were prepared based on the optimal formulation. The release profile, biodegradability and mechanical properties of the wound dressings were assessed. The antibacterial property of Ag/gCN/EE was studied demonstrating strong antibacterial activity on <em>E. coli</em> and <em>S. aureus</em>. MTT assay was carried out on NIH 3T3 fibroblast cells, and BC/Ag/gCN/EE and PVA/BC/Ag/gCN/EE nanocomposites showed 89 ± 2.31 % and 96 ± 3.28 % viability, respectively and no toxicity. To assess the effect of the composites on <em>in vitro</em> wound healing and cell migration, scratch wound assay was performed. The results indicated that after 24 h, BC/Ag/gCN/EE and PVA/BC/Ag/gCN/EE reduced 18.69 and 23.97 % of the scratch area compared to the control group. The prepared composites are promising wound dressings that could accelerate wound healing and kill bacteria simultaneously.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100190"},"PeriodicalIF":0.0,"publicationDate":"2024-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000621/pdfft?md5=225ca1684251721da5076d8a548db09e&pid=1-s2.0-S2772417424000621-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141695547","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"N-isopropyl-(4-methoxy-3-difluoromethyl)cinnamoyl amide targets mycobacterial MmpL3","authors":"Mario D. Martínez ,&nbsp;Liliana Rondón ,&nbsp;Lisandro Ronconi ,&nbsp;Mariano Prado Acosta ,&nbsp;Agostina Crotta Asis ,&nbsp;Gabriela Gago ,&nbsp;Florencia Di Salvo ,&nbsp;Gerardo Burton ,&nbsp;Fernando Durán ,&nbsp;Mariana Piuri","doi":"10.1016/j.ejmcr.2024.100188","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100188","url":null,"abstract":"<div><p>Mycobacterial infections still need new and more efficient drugs. In the present work we developed a new and simpler protocol for the synthesis of <em>N</em>-isopropyl-(4-methoxy-3-difluoromethyl)cinnamoyl amide, here named as 3M99F1, a promising candidate for mycobacterial growth inhibition. Using whole genome sequencing of 3M99F1 resistant strains we were able to identify Mycobacterial membrane protein Large 3 (MmpL3) as the target for this compound. MmpL3 inhibition by 3M99F1 was further confirmed by lipid analysis of Mycobacteria in the presence and absence of the drug. MmpL3 is well conserved in <em>Mycobacteria,</em> including atypical or NTM (non-tuberculous mycobacteria) and other Actinobacteria<em>,</em> but it is not present in humans, encouraging the development of new inhibitors using 3M99F1 as scaffold.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100188"},"PeriodicalIF":0.0,"publicationDate":"2024-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000608/pdfft?md5=4d34f9e993ba010f2df52d94fe944896&pid=1-s2.0-S2772417424000608-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141607744","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design, synthesis and biological Evaluation of novel chromones having 3,4-dihydropyrimidin-2(1H)-one core at C-8 in combination with triazoles: New α-glucosidase inhibitors and anti-bacterial agents","authors":"Kumara Swamy Taviti ,&nbsp;T.B. Patrudu ,&nbsp;Nagalakshmi Jeedimalla ,&nbsp;Naresh Kumar Katari ,&nbsp;Satyanarayana Yatam ,&nbsp;Rambabu Gundla","doi":"10.1016/j.ejmcr.2024.100187","DOIUrl":"10.1016/j.ejmcr.2024.100187","url":null,"abstract":"<div><p>The Biginelli reaction synthesizes dihydropyrimidones through a multi-component reaction. A β-ketoester, aldehyde, and urea or thiourea react in the presence of an acid catalyst to form these dihydropyrimidones. 3,4-Dihydropyrimidin-2(1H)-One/Chromone/Triazole hybrids (<strong>9a-9l</strong>) were synthesized by multiple steps including one pot Biginelli multicomponent reaction depicted in the scheme. An efficient method for the Biginelli reaction of Chromone aldehyde, acetoacetate esters, and urea employed in the presence of ferric chloride is described. In the end, we have successfully synthesized twelve derivatives of 3,4-Dihydropyrimidin-2(1H)-One/Chromone/Triazole hybrids and subjected them to testing for Antibacterial activity and α-glucosidase inhibition activity. Among these derivatives, compound <strong>9g</strong> (IC50 = 142.92 nmol) and <strong>9e (</strong>144.49 nmol<strong>)</strong> exhibited significant inhibitory activity in comparison to the positive control acarbose (IC50 = 350.91 nmol). Compound <strong>9g</strong> demonstrated the most significant suppression against <em>Escherichia coli</em> and <em>Bacillus cereus</em>, with zone diameters of 8.8 ± 1.35 mm and 9.1 ± 0.23 mm, respectively. Compound 9b displayed a clear area where bacterial growth was inhibited, measuring 7.5 ± 1.25 mm against <em>Klebsiella pneumonia</em>. Compound 9k exhibited a zone of inhibition measuring 8 ± 1.2 mm in radius against <em>Staphylococcus epidermidis</em>. The docking results for the synthesized compounds indicate that compound 9b exhibited the most favorable docking score of −10 kcal/mol, whereas compound <strong>9a</strong> had the second-best docking score of −8.7 kcal/mol. Molecular docking was utilized to examine the interactions between the title compounds and α-glucosidase, in order to provide valuable insights. The data obtained revealed significant interactions that contribute to the inhibitory effects of the drugs against α-glucosidase. These compounds exhibit significant potential as attractive initial candidates for the development of new α-glucosidase inhibitors.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100187"},"PeriodicalIF":0.0,"publicationDate":"2024-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000591/pdfft?md5=1e1d581a506b838ceac7ffb9677dd604&pid=1-s2.0-S2772417424000591-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141960883","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Propofol orchestrates long non-coding RNAs in MCF7 cells, unraveling new avenues for breast cancer intervention","authors":"Cigir Biray Avci ,&nbsp;Tuba Gokdogan Edgunlu ,&nbsp;Tugba Suzek ,&nbsp;Neslihan Pinar Ozates ,&nbsp;Bakiye Goker Bagca ,&nbsp;Aysegul Demirtas Bilgic ,&nbsp;Cilem Ozdemir ,&nbsp;Bakiye Ugur","doi":"10.1016/j.ejmcr.2024.100186","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100186","url":null,"abstract":"<div><p>Long non-coding RNAs (lncRNAs) play a dynamic role in gene expression regulation and serve as potential therapeutic targets in breast cancer. The anticancer effect of propofol, an anesthetic agent, has been proven, but its interaction with lncRNAs has not been adequately investigated. This study aims to reveal the interactions between propofol and lncRNAs and contribute to the understanding of its therapeutic potential in the treatment of breast cancer. We evaluated the effects of propofol on cell viability, apoptosis, and mitochondrial membrane potential in MCF7 cells. The study used qRT-PCR to analyze cancer-related lncRNA expressions following propofol treatment; this was supported by RNA-RNA interaction predictions and in silico functional analysis using selected datasets and the R cluster Profiler GSEABase package. Propofol showed a cytotoxic effect at higher doses in MCF7 breast cancer cells, inducing necrosis. Propofol regulated (IGF2-AS, MRPL23-AS1, PANDAR, HULC) and down-regulated (IWT1-AS, HOXA-AS2, H19, GACAT1, MIAT) the expression levels of various lncRNAs in MCF7 cells. Our research revealed complex interactions of MALAT1 lncRNA with both upregulated and downregulated genes. Additionally, three rRNA genes (LSU-rRNA, RNA45SN3, and SSU-rRNA) were identified to interact with both groups of lncRNAs. Propofol potentially targets chemotherapy resistance by regulating UCA1, LINC-RoR1, and MEG3. Wikipathways' pathway enrichment analysis identified two downregulated lncRNAs, UCA1 and LINC-RoR1, and an upregulated MEG3, implicated in lncRNA-mediated chemotherapeutic resistance mechanisms. Our study illuminates the intricate interplay of lncRNAs and their potential contribution to propofol's anti-cancer effects in breast cancer, offering new avenues for therapeutic exploration and advancement.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100186"},"PeriodicalIF":0.0,"publicationDate":"2024-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S277241742400058X/pdfft?md5=9bba3576e43145de0501adcd00d5b4f7&pid=1-s2.0-S277241742400058X-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141582750","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Recent advancements in the synthesis of fused thienopyridines and their therapeutic applications","authors":"Ranjay Shaw ,&nbsp;Ritu Tewari ,&nbsp;Monika Yadav ,&nbsp;Ekta Pandey ,&nbsp;Khyati Tripathi ,&nbsp;Jyoti Rani ,&nbsp;Ismail Althagafi ,&nbsp;Ramendra Pratap","doi":"10.1016/j.ejmcr.2024.100185","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100185","url":null,"abstract":"<div><p>Fused thienopyridines represent a class of heterocyclic molecules that have garnered increasing attention due to their unique structural features and versatile chemical properties. This review systematically examines the latest synthetic methodologies employed in preparing fused thienopyridine derivatives, emphasizing innovative approaches that contribute to structural diversity. Moreover, the discussion extends to the broad spectrum of therapeutic applications that fused thienopyridines offer, encompassing their utility in different diseases. The review explores the pharmacological activities and biological properties of fused thienopyridines, shedding light on their role in drug discovery and development. By offering a comprehensive overview of recent advancements in both the chemical synthesis and therapeutic applications of fused thienopyridines, this review will serve as a valuable resource for researchers and practitioners navigating the evolving landscape of medicinal chemistry.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100185"},"PeriodicalIF":0.0,"publicationDate":"2024-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000578/pdfft?md5=3322cc736ef749b485568f4dfb60d3dc&pid=1-s2.0-S2772417424000578-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141540276","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Thiadiazole-thiazole derivatives as potent anti-tubercular agents: Synthesis, biological evaluation, and In silico docking studies","authors":"Samin A. Shaikh ,&nbsp;Shivaji R. Labhade ,&nbsp;Raju R. Kale ,&nbsp;Prajakta Y. Pachorkar ,&nbsp;Rohan J. Meshram ,&nbsp;Kamlesh S. Jain ,&nbsp;Hrishikesh S. Labhade ,&nbsp;Dipak D. Bhanushali ,&nbsp;Rahul A. More ,&nbsp;Charushila K. Nerkar ,&nbsp;Santosh S. Chobe ,&nbsp;Aniket N. Marathe ,&nbsp;Satish N. Wakchaure ,&nbsp;Deepak R. Boraste","doi":"10.1016/j.ejmcr.2024.100183","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100183","url":null,"abstract":"<div><p>The present study focuses on research findings related to the development and assessment of thiadiazole-linked thiazole derivatives as promising anti-tubercular agents. We present the synthesis data of eleven new compounds (<strong>4a-4k</strong>) and confirm their structures using spectroscopic techniques. Subsequently, the compounds were screened for their anti-tuberculosis activities against <em>M. tuberculosis</em> H37Ra. The results demonstrated that compounds <strong>3</strong> and <strong>4b</strong> exhibited minimum inhibitory concentration (MIC) of <strong>3.90 μg/mL</strong> and <strong>7.81 μg/mL</strong>, respectively. <em>In-vitro</em>, studies for few compounds exhibited high antioxidant activity against DPPH and OH radical scavengers along with minimal to no cytotoxicity against RBCs which is a promising result. Investigation of molecular docked conformations revealed different molecular interactions such as hydrogen bonds, halogen bonds, and interactions involving Pi electron cloud. The study sheds light on conserved interactions with residues like Met131, Val163, His90 and Gln161 from the tubercular MCAT enzyme. Interestingly, the synthetic chemistry reveals that the employment of tetra-n-butylammonium bromide (TBAB) plays a crucial role for N-butylation and it also expedites the reaction in tetrahydrofuran solvent.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100183"},"PeriodicalIF":0.0,"publicationDate":"2024-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000554/pdfft?md5=6940dda42c380e790c15e3dc0ecff4ac&pid=1-s2.0-S2772417424000554-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141582749","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Polyphenol encapsulated nanofibers in wound healing and drug delivery","authors":"Ovinuchi Ejiohuo ,&nbsp;Samson O. Folami ,&nbsp;Deinmo Edi ,&nbsp;Jessica Isaac","doi":"10.1016/j.ejmcr.2024.100184","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100184","url":null,"abstract":"<div><p>Polyphenol is a versatile green phytochemical vital in several biomedical applications with fascinating inherent biocompatible, bioadhesive, antioxidant, and antibacterial properties. The emergence of novel nanotechnology techniques, such as electrospinning, has proven to be an excellent option for applications in nanotechnology, ensuring an effective drug delivery system for recognised medicinal plant extracts containing polyphenols as electrospun nanofibers can provide the necessary environment for encapsulation. Together, electrospun nanofibers and polyphenols have shown promising usage in wound healing. When polyphenols are incorporated into nanofibrous scaffolds, their combined properties enhance cell attachment, proliferation, and differentiation. This review explores the potential of polyphenol-loaded nanofibers for wound therapy, highlighting the importance of efficient drug delivery systems for electrospun polyphenols. It provides a brief assessment of specific polyphenols (resveratrol, curcumin, thymol, quercetin, tannic acid, ferulic acid, hesperidin, gallic acid, kaempferol, chlorogenic acid) that have been successfully encapsulated in electrospun nanofibers and applied in wound treatment. Despite ongoing research, certain polyphenols such as carvacrol, oleuropein, chlorogenic acid, gallic acid, and kaempferol in electrospun nanofibers remain less explored. This review underscores the need for continued investigation into these promising systems while recognising the growing application of polyphenol-loaded nanofibers in wound healing and their potential for more extensive therapeutic use.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100184"},"PeriodicalIF":0.0,"publicationDate":"2024-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000566/pdfft?md5=89ed9a1b2c53655bada4e15145a34552&pid=1-s2.0-S2772417424000566-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141484484","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and experimental validation of a new radiolabeled analog of N-(3-hydroxy-4-methoxy-phenyl-methyl) ferrocene-carboxamide (VFC) targeting the TRPV1 receptor","authors":"Tesnim Dallegi ,&nbsp;Syrine Ben Hassen ,&nbsp;Nedra Rached ,&nbsp;Farah Menjji ,&nbsp;Roufaida Abassi ,&nbsp;Ameur Cherif ,&nbsp;Soumaya Kouidhi ,&nbsp;Mouldi Saidi ,&nbsp;Amor Mosbah","doi":"10.1016/j.ejmcr.2024.100182","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100182","url":null,"abstract":"<div><p>The TRPV1 receptor has been recognized to play a role in cancer development, being overexpressed in prostate, breast, lung, and colon cancers. Since TRPV1 activation promotes cancer cell proliferation, invasion, and migration, TRPV1 antagonists may show potential as anti-cancer agents. Capsaicin and capsaicinoids are phytochemicals derived from homovanillic acid found in abundance in chili peppers and responsible for its pungent properties. Capsaicin acts as a potent agonist of TRPV1 with recognized antineoplastic properties. Here, we employ computational approaches including molecular modeling and docking to refine the 3D structure of human TRPV1 and assess its interaction with the newly synthesized N-(3-hydroxy-4-methoxyphenylmethyl)ferrocenecarboxamide (VFC) and its cyclopentadienyl tricarbonyl rhenium and technetium analogs. Radiolabeling of VFC with ^99mTc was achieved by double ligand exchange to afford ^99mTc-VFC in high radiochemical purity and yield. Biodistribution studies in mice demonstrated preferential accumulation of ^99mTc-VFC in the bladder, liver, kidney, and lung. These findings may contribute to developing efficient TRPV1-targeted radiotracers for molecular imaging of tumors by SPECT.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100182"},"PeriodicalIF":0.0,"publicationDate":"2024-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000542/pdfft?md5=a423b180f679e40060165ab4ec98c2ad&pid=1-s2.0-S2772417424000542-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141484481","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of anthelmintic and antioxidant efficacy of green-synthesized copper nanoparticles derived from Erioglossum rubiginosum leaf and seed aqueous extracts","authors":"Md. Al-Imran Imon ,&nbsp;Sharmin Nur Toma ,&nbsp;S.M. Sohag ,&nbsp;Md. Jakaria Islam ,&nbsp;Md. Monirul Islam ,&nbsp;Md. Shihab Uddin Sohag ,&nbsp;Imran Mahmud ,&nbsp;Naznin Shahria ,&nbsp;Sanjay Dutta","doi":"10.1016/j.ejmcr.2024.100181","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100181","url":null,"abstract":"<div><p>The green synthesis of copper nanoparticles refers to the preparation of nanoparticles using eco-friendly and sustainable processes, often involving plant extracts, microorganisms, or other natural sources. As a sustainable approach with many potential applications, plant extracts could be used for the green synthesis of copper nanoparticles. The green synthesis of copper nanoparticles from plants, such as <em>Erioglossum rubiginosum,</em> involves using leaf and seed extracts to reduce copper ions to form nanoparticles. Primarily, copper nanoparticles are confirmed by visual observation of the aluminum vessel’s inner wall exhibiting a glossy, reddish-brown precipitate. Further, the UV–Vis spectrophotometer is employed to detect the presence of CuNPs. The peak is at 631 nm, which is unique to CuNPs. FTIR data show the presence of a capping agent which stabilizes copper nanoparticles. The peaks at 3,265 cm⁻¹ for the hydroxy group (H-bonded OH stretch) indicate alcohols and phenols; 1610 cm⁻¹ for aromatic ring stretch; and 1,075 cm⁻¹ for aliphatic fluoro compounds (C–F stretch). DPPH reducing power assay is used to verify the antioxidant activity. Both plant extracts and the synthesized CuNPs showed considerable antioxidant activity. The seed and leaf extract of <em>Erioglossum rubiginosum</em> used for the green synthesis of copper nanoparticles served as a capping agent due to the presence of antioxidant phytoconstituents. Then, we used <em>Paramphistomum cervi</em> to evaluate the anthelmintic activity of aqueous extracts of leaves and seeds of <em>Erioglossum rubiginosum</em>. After that, we assessed the anthelmintic activity of the green synthesized copper nanoparticles (CuNPs). We observed that the extracts showed a significant and dose-dependent decrease in the paralysis time and death time of parasites whereas better activity was found from the synthesized CuNPs. At last, we claim that comprehensive investigation on plant extracts and CuNPs could be carried out for further study and might pave the way for development of novel therapeutic agents that show efficacy against diverse parasitic infections.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100181"},"PeriodicalIF":0.0,"publicationDate":"2024-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000530/pdfft?md5=112b3af2f838039e1ee7db79a40aee73&pid=1-s2.0-S2772417424000530-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141484483","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Chromone hybrids as interleukin-6 and acetylcholinesterase inhibitor for treatment of Alzheimer's disease: Design, docking, synthesis and evaluation","authors":"Shivam Mishra,&nbsp;Sukhvir Kaur,&nbsp;Gulshan Bansal,&nbsp;Yogita Bansal","doi":"10.1016/j.ejmcr.2024.100180","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100180","url":null,"abstract":"<div><p>The course of Alzheimer's disease (AD) is largely influenced by interleukin-6 (IL-6) and acetylcholinesterase (AChE). Therefore, concurrent suppression of these two targets is a rational approach for the development of anti-AD molecules. The study is aimed to design a molecule with pharmacophore capable of inhibiting both the targets. Four series are designed by coupling a chromone moiety (a pharmacophore that inhibits IL-6) with a N,N-disubstituted amine (that inhibits AChE) through a linker (1–4 carbon chain). The <em>in silico</em> studies on the designed compounds led to the identification of 16 best-fit compounds having good oral bioavailability and blood brain barrier permeability. All 16 compounds were synthesized and evaluated for anti-AChE activity. Six compounds showing &gt;45 % inhibition of AChE at 1 μM concentration are further evaluated for BuChE (butyrylcholinesterase) and IL-6 inhibitory activities. Compound YS3g is the most potent inhibitor of <em>Ee</em>AChE (IC₅₀ = 0.45 μM) and of IL-6 (IC₅₀ = 0.46 μM). Subsequently, it is found to show dose-dependent effects in STZ (streptozotocin)-induced memory deficit model at three doses (0.2, 0.4 and 0.8 mg/kg). At higher dose (0.8 mg/kg), it reverses the deficit as also supported by histopathological studies. The findings reveal that a chromone nucleus coupled with a piperazine via a three-carbon linker may be a useful template for developing novel moieties against AD.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100180"},"PeriodicalIF":0.0,"publicationDate":"2024-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000529/pdfft?md5=aba3c43ff2e3c43ceeb763d9dc7b1dcb&pid=1-s2.0-S2772417424000529-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141484485","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}