European Journal of Medicinal Chemistry Reports最新文献

{"title":"The pyrazolo[4,3-c]pyrazole core as a novel and versatile scaffold for developing dual DYRK1A-CLK1 inhibitors targeting key processes of Alzheimer's disease pathology","authors":"Vaia-Argyro Bakalakou ,&nbsp;Barbara Mavroidi ,&nbsp;Amalia D. Kalampaliki ,&nbsp;Béatrice Josselin ,&nbsp;Stéphane Bach ,&nbsp;Alexios-Leandros Skaltsounis ,&nbsp;Panagiotis Marakos ,&nbsp;Nicole Pouli ,&nbsp;Maria Pelecanou ,&nbsp;Vassilios Myrianthopoulos ,&nbsp;Sandrine Ruchaud ,&nbsp;Ioannis K. Kostakis","doi":"10.1016/j.ejmcr.2024.100193","DOIUrl":"10.1016/j.ejmcr.2024.100193","url":null,"abstract":"<div><p>In the current study, we designed, synthesized, and characterized a series of substituted pyrazolo[4,3-<em>c</em>]pyrazoles. These novel compounds were evaluated <em>in vitro</em> for their inhibitory activity over a panel of protein kinases to determine their potential therapeutic applications against Alzheimer's disease. To gain deeper insight into the binding interactions between the most potent analogues and their respective kinase targets, advanced molecular simulations were performed. In parallel, the ability of pyrazolo[4,3-<em>c</em>]pyrazoles to inhibit Aβ40 aggregation was assessed using biophysical techniques such as circular dichroism and Thioflavin T assays. Our results highlight the specific heterocycle as a highly promising and synthetically versatile scaffold for developing inhibitors of both AD-relevant kinases and amyloid-β aggregation. Although more effort is needed to assess the possibility of developing multi-target inhibitors, pyrazolo[4,3-<em>c</em>]pyrazole analogues demonstrated significant activities against their individual targets, indicating substantial capacity of the heterocyclic scaffold for further optimization toward both directions. Overall, our findings emphasize the potential of properly substituted pyrazolo[4,3-<em>c</em>]pyrazoles as multifunctional agents targeting key processes in Alzheimer's disease pathology.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100193"},"PeriodicalIF":0.0,"publicationDate":"2024-07-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000657/pdfft?md5=002c3aff6565dd193d3d19fb0567762c&pid=1-s2.0-S2772417424000657-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141846847","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":"Current status of 1,4-Naphthoquinones and their derivatives for wound healing","authors":"Pooja Kumari ,&nbsp;Vikramjeet Singh ,&nbsp;Vinay Kant ,&nbsp;Munish Ahuja","doi":"10.1016/j.ejmcr.2024.100194","DOIUrl":"10.1016/j.ejmcr.2024.100194","url":null,"abstract":"<div><p>Cutaneous wounds are a major healthcare concern affecting millions of people as they fail to heal properly and can result in life threatening conditions and high economic loss. Wound healing is a complex, multifaceted process involving four consequent stages: haemostasis, inflammation, proliferation, and tissue remodelling. These phases work in coordination to restore the integrity of damaged skin and underlying tissues. 1,4-Naphthoquinone compounds and their derivatives have emerged as promising candidates in wound management. Herein, natural compounds such as lawsone, juglone, shikonin, plumbagin along with their derivatives have been discussed for wound healing potential with special emphasis on structural activity relationships. This review provides a comprehensive discussion on the chemical reactivity, biological activities, and mechanisms of action of these naphthoquinone-based compounds, particularly their antibacterial properties, which play a crucial role in wound healing. The review highlights the importance of elucidating structure-activity relationships to overcome challenges associated with poor solubility, low antibacterial efficacy, and the presence of inevitable impurities in plant extracts. Additionally, the review emphasizes the significance of developing diverse naphthoquinone derivatives at the laboratory scale to expand the repertoire of potential wound healing agents.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100194"},"PeriodicalIF":0.0,"publicationDate":"2024-07-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000669/pdfft?md5=1e1bdf02aeea0b615e24967ce00fbced&pid=1-s2.0-S2772417424000669-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141843219","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":"Antimicrobial effects of new tetrahydrofurans","authors":"Shanmugha Samy ,&nbsp;Manikandan Alagumuthu ,&nbsp;Milind Shrinivas Dangate","doi":"10.1016/j.ejmcr.2024.100191","DOIUrl":"10.1016/j.ejmcr.2024.100191","url":null,"abstract":"<div><p>The increasing challenge of antimicrobial resistance (AMR) necessitates abrupt attention to discovering a new class of antimicrobials. In this study, we made efforts to prepare some fluoro-phenyl tetrahydrofurans-based DNA gyrase inhibitors as anti-microbial agents. To obtain the title compounds difluoro phenyl tetrahydrofurans (<strong>1-12</strong>), we used fluorophenyl-tetrahydrofuran and methyl benzenesulfonate to react with isoxazole derivatives and heterocyclic compounds bearing secondary amines in the presence of dimethylformamide (DMF) and sodium hydride (NaH) or potassium carbonate (K₂CO₃). The compounds were obtained in moderate to excellent yields and were characterized with FTIR, HRMS, NMR, etc. Among all compounds (<strong>1-12</strong>), compounds <strong>1, 2, 11,</strong> and <strong>12</strong> were active against various Gram-positive and Gram-negative bacteria at a low concentration (MIC ranged between 1.25 and 9.75 μg/mL) and displayed low toxicity towards mammalian cells. We testified the <em>in vitro</em> DNA gyrase inhibitory potential for these compounds. A molecular docking study and an ADMET assessment study were carried out to understand the mode of interaction of ligand-DNA gyrase. In conclusion, we screened the compounds <strong>1, 2, 11,</strong> and <strong>12</strong> for further clinical and pre-clinical studies.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100191"},"PeriodicalIF":0.0,"publicationDate":"2024-07-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000633/pdfft?md5=4f2a370c52787ef72459a9b5cfa2f867&pid=1-s2.0-S2772417424000633-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141851818","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":"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}