RSC AdvancesPub Date : 2025-01-22DOI: 10.1039/D4RA09017A
Bilal Nehmeh, Fatima Haydous, Hiba Ali, Adonis Hdaifi, Bayan Abdlwahab, Mariam Bou Orm, Zohrab Abrahamian and Elias Akoury
{"title":"Emerging contaminants in the Mediterranean Sea endangering Lebanon's Palm Islands Natural Reserve†","authors":"Bilal Nehmeh, Fatima Haydous, Hiba Ali, Adonis Hdaifi, Bayan Abdlwahab, Mariam Bou Orm, Zohrab Abrahamian and Elias Akoury","doi":"10.1039/D4RA09017A","DOIUrl":"https://doi.org/10.1039/D4RA09017A","url":null,"abstract":"<p >The Mediterranean Sea is an intercontinental marine environment renowned for its biodiversity and ecological significance. However, it is also one of the most polluted seas globally with significant levels of microplastics and heavy metals among other emerging contaminants. In Lebanon, inadequate waste management infrastructure and unregulated industrial discharges have exacerbated water quality deterioration by introducing these complex contaminants into surface and seawater. The Palm Islands Natural Reserve in Lebanon is a UNESCO-designated marine protected area and home to endangered species. However, the reserve faces significant threats from pollution, including heavy metals and microplastics, exacerbated by nearby Tripoli's escalating contamination. Plasticisers, particularly phthalates, are recognized for their hormone-disrupting effects, and heavy metals like cadmium, lead, and arsenic pose severe eco-toxicological risks. This study investigates the levels of heavy metals and phthalates in water and sediments from the Palm Islands. Samples were collected from different locations within the reserve, and heavy metals and phthalates were detected, including chromium (13.58 to 19.28 μg L<small><sup>−1</sup></small>), arsenic (2.05 to 5.04 μg L<small><sup>−1</sup></small>), cadmium (1.27 to 3.04 μg L<small><sup>−1</sup></small>), and lead (0.92 to 2.88 μg L<small><sup>−1</sup></small>). Cadmium levels exceeded the permissible limits set by environmental regulatory bodies, highlighting an urgent pollution problem. Phthalates, including DEP and DEHP, were also detected in concentrations of 7.12–10.25 μg L<small><sup>−1</sup></small> for DEP and 38.47–56.12 μg L<small><sup>−1</sup></small> for DEHP raising concerns over their potential eco-toxicological impact on marine species. Our research underscores the need for comprehensive environmental monitoring, better waste management infrastructure, and stricter regulatory measures to address pollution in Lebanon's coastal ecosystems.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 2034-2044"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra09017a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994291","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2025-01-22DOI: 10.1039/D4RA07294D
A. Niranjana Kumar, Smruti Ranjan Das, J. Kotesh Kumar, K. V. N. S. Srinivas and Sarada D. Tetali
{"title":"Design and development of an isatin-1,2,3-triazole hybrid analogue as a potent anti-inflammatory agent with enhanced efficacy and gene expression modulation†","authors":"A. Niranjana Kumar, Smruti Ranjan Das, J. Kotesh Kumar, K. V. N. S. Srinivas and Sarada D. Tetali","doi":"10.1039/D4RA07294D","DOIUrl":"https://doi.org/10.1039/D4RA07294D","url":null,"abstract":"<p >Isatin (1<em>H</em>-indole-2,3-dione) and its derivatives have been found to exhibit various biological activities, including anticancer and antidiabetic properties. In this study, a series of nine isatin-1,2,3-triazole conjugates were synthesized and evaluated for their anti-inflammatory potential <em>via in vitro</em> experiments. Their synthesis involved the propargylation of isatin <strong>1</strong> with propargyl bromide to obtain <em>N</em>-propargyl isatin <strong>2</strong>, which was subjected to click reactions with different aromatic azides to yield isatin-<em>N</em>-1,2,3-triazoles (<strong>3a–i</strong>). The structures of all the compounds were confirmed <em>via</em> NMR and HR-MS. The final isatin analogues were tested for their ability to attenuate the production of proinflammatory cytokines in the lipopolysaccharide (LPS)-induced human leukemia monocytic THP-1 cells. Importantly, none of the compounds had any negative effect on THP-1 cell viability at the tested concentrations of 4 mM and 8 mM. LPS induced the production of the cytokines: Tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) and monocyte chemoattractant protein-1 (MCP-1) by 351.4, 7.9 and 14.3 fold, respectively, in THP-1 cells. However, treatment with compound <strong>3e</strong> markedly attenuated the levels of TNF-α (by 6.6 fold and 1.5 fold), IL-6 (by 1.03 fold and 1.41 fold) and MCP-1 (by 3.3 fold and 1.7 fold) by several fold at concentrations of 4 mM and 8 mM, respectively. Furthermore, in the gene expression modulation studies, <strong>3e</strong> was found to downregulate the genes responsible for the production of TNF-α (24 and 25 fold), IL-6 (148 and 502 fold) and MCP-1 (50 and 25 fold) at the two tested concentrations compared with their expression in the LPS-induced THP-1 cells (135 fold, 6612 fold, and 68.8 fold, respectively). Thus, <strong>3e</strong> markedly attenuated the secretion of TNF-α, IL-6 and MCP-1 from LPS-treated THP-1 cells, and also the expression of the concerned genes. At the lowest dose tested, <em>i.e.</em>, 4 mM, <strong>3e</strong> had the greatest effect on both gene expression and marker secretion.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 2023-2033"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra07294d?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994290","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2025-01-22DOI: 10.1039/D4RA08032G
Samira Husen Alamudi and Yong-An Lee
{"title":"Design strategies for organelle-selective fluorescent probes: where to start?","authors":"Samira Husen Alamudi and Yong-An Lee","doi":"10.1039/D4RA08032G","DOIUrl":"https://doi.org/10.1039/D4RA08032G","url":null,"abstract":"<p >Monitoring physiological changes within cells is crucial for understanding their biological aspects and pathological activities. Fluorescent probes serve as powerful tools for this purpose, offering advantageous characteristics over genetically encoded probes. While numerous organelle-selective probes have been developed in the past decades, several challenges persist. This review explores the strategies and key factors contributing to the successful rationale design of these probes. We systematically discuss the typical mode of cellular uptake generally adopted by fluorescent probes and provide a detailed examination of the key factors to consider in design rationale from two perspectives: the properties of the target organelle and the physicochemical properties of the probe itself. Additionally, recent examples of organelle-targeted probes are presented, along with a discussion of the current challenges faced by fluorescent probes in the field.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 2115-2131"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra08032g?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994297","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"The effect of feedstock concentration on the crystal phase, morphology, and optical properties of WO3 nanostructures†","authors":"Mohsen Zafari, Fatemeh Shariatmadar Tehrani, Seyed Hossein Hosseini Shokouh, Alexey Popov and Krisztian Kordas","doi":"10.1039/D4RA07112C","DOIUrl":"https://doi.org/10.1039/D4RA07112C","url":null,"abstract":"<p >In this study, the effect of feedstock concentration on the synthesis of WO<small><sub>3</sub></small> nanostructures in a one-step hydrothermal process was investigated. According to our experiments, when titrating aqueous Na<small><sub>2</sub></small>WO<small><sub>4</sub></small>·2H<small><sub>2</sub></small>O with HCl solutions of different concentrations to a constant pH of 1.5, after identical hydrothermal treatments at 180 °C, the morphology, crystal size and phase composition as well as the optical properties of the products could be tuned. Furthermore, by applying Na<small><sub>2</sub></small>SO<small><sub>4</sub></small> in the precursor solution, we get a further degree of freedom to alter the structural and optical properties of the products. The precursor concentration dependent optical band gap energy values (that vary from ∼2.5 eV to ∼2.9 eV) are in good agreement with the associated hexagonal (from 32.7% to 65.5%) and orthorhombic (from 67.3% to 34.5%) phases of nanostructured tungsten oxide products. The calculated Urbach energies can be well explained by the oxygen deficient crystals. The latter is also coherent with measured photoluminescence (multiple peaks between 400 and 580 nm) that indicate abundant defect states in the tungsten oxide products.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 2099-2105"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra07112c?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994295","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2025-01-22DOI: 10.1039/D4RA08139K
Mohsin Javed, Afzal Shah and Muhammad Umar Farooq
{"title":"An electroanalytical sensor for the detection of antibiotic cefoperazone sodium sulbactam sodium residue in wastewater","authors":"Mohsin Javed, Afzal Shah and Muhammad Umar Farooq","doi":"10.1039/D4RA08139K","DOIUrl":"https://doi.org/10.1039/D4RA08139K","url":null,"abstract":"<p >The misuse and uncontrolled release of pharmaceuticals into water bodies lead to environmental challenges and the development of resistance, thereby reducing their effectiveness. To mitigate these problems, it is essential to identify pharmaceuticals in water sources and eliminate them prior to human use. This study presents the designing of a novel nanosensor for the detection of the antibiotic Cefoperazone Sodium Sulbactam Sodium (CSSS). The nanosensor was prepared by modifying the surface of a glassy carbon electrode (GCE) with the nanoparticles of NiO and MWCNTs. A green synthetic method was applied for the synthesis of NiO nanoparticles. Their structural and morphological characterization was conducted using X-ray diffraction and scanning electron microscopy, while optical properties were assessed through UV-vis spectroscopy. NiO nanoparticles in conjunction with MWCNTs enhanced the sensitivity of the GCE for the detection of CSSS. Electrochemical impedance spectroscopy revealed efficient charge transport through the designed sensing platform designated as NiO/MWCNTs/GCE. Square wave voltammetry demonstrated an eightfold increase in peak current intensity of CSSS at the NiO/MWCNTs/GCE as compared to the unmodified GCE. The electrochemical analysis of CSSS in solution of different pH indicated the involvement of protons during electron transfer reactions of CSSS. The limit of detection of CSSS with a value of 3.31 nM was obtained at the designed sensing platform under optimized experimental conditions. The current investigations combine advanced materials with principles of green chemistry, significantly enhancing efforts in wastewater remediation from antibiotic drugs.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 2011-2022"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra08139k?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994285","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2025-01-22DOI: 10.1039/D4RA07123A
Md. Akhtarul Alam, Anamika Hoque, Md Sanaul Islam, Nargis Khatun, Manash Pratim Sarmah, A. K. M. Maidul Islam, Manabendra Sarma, Goutam Kumar Kole and Ennio Zangrando
{"title":"An electrically conductive dinuclear aluminium complex for the fabrication of a Schottky diode","authors":"Md. Akhtarul Alam, Anamika Hoque, Md Sanaul Islam, Nargis Khatun, Manash Pratim Sarmah, A. K. M. Maidul Islam, Manabendra Sarma, Goutam Kumar Kole and Ennio Zangrando","doi":"10.1039/D4RA07123A","DOIUrl":"https://doi.org/10.1039/D4RA07123A","url":null,"abstract":"<p >Electrical performances of a biphenyl-derived amido Schiff base ligand <strong>L</strong> and its dinuclear Al(<small>III</small>) complex (complex <strong>1</strong>) were investigated in a metal–semiconductor (MS) junction. Electrical studies revealed that complex <strong>1</strong> significantly enhanced the electrical conductivity and improved the characteristics of a Schottky barrier diode (SBD). The <em>I</em>–<em>V</em> characteristics demonstrated that complexation of ligand <strong>L</strong> with Al(<small>III</small>) ion increased the conductivity by two orders of magnitude (conductivity of <strong>L</strong> = 1.04 × 10<small><sup>−7</sup></small> Sm<small><sup>−1</sup></small> and complex <strong>1</strong> = 1.04 × 10<small><sup>−5</sup></small> Sm<small><sup>−1</sup></small>) with improved diode rectification ratio. Complex <strong>1</strong> extended itself to the 3D supramolecular array by virtue of the hydrogen bond, C–H⋯π(C) bond and π⋯π interactions. This significantly influenced the semiconducting behaviour of complex <strong>1</strong> and essentially improved the characteristics of SBD. The optical band gap of complex <strong>1</strong> and ligand <strong>L</strong> in the solid state was determined experimentally (2.63 eV and 3.04 eV, respectively) and compared with the theoretical value obtained from DFT calculations. Furthermore, DOS analysis explained the conductivity behavior of complex <strong>1</strong> in a logically better way.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 2132-2139"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra07123a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994298","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2025-01-22DOI: 10.1039/D4RA07622B
Ondřej Zapadlík, Jan Pejchal, Vladimir Babin, Vítězslav Jarý, Vojtěch Vaněček, Romana Kučerková, Karel Jurek, Alena Beitlerová and Martin Nikl
{"title":"GSAG:Ce scintillator: insights from yttrium admixture†","authors":"Ondřej Zapadlík, Jan Pejchal, Vladimir Babin, Vítězslav Jarý, Vojtěch Vaněček, Romana Kučerková, Karel Jurek, Alena Beitlerová and Martin Nikl","doi":"10.1039/D4RA07622B","DOIUrl":"https://doi.org/10.1039/D4RA07622B","url":null,"abstract":"<p >The GSAG:Ce scintillator represents a promising and cost-effective alternative to the expensive GGAG:Ce. Recent studies have attributed its low light yield to the thermal quenching effect. In this study, we employed the strategy of adding an yttrium (Y) admixture to the GSAG matrix to increase the thermal activation energy of thermal quenching. The scintillation, optical, and luminescence properties of Gd<small><sub>(3−<em>x</em>)</sub></small>Y<small><sub><em>x</em></sub></small>Sc<small><sub>2</sub></small>Al<small><sub>3</sub></small>O<small><sub>12</sub></small>:Ce (<em>x</em> = 0, 0.2, 0.5, 0.8) grown using the micro-pulling-down method are thoroughly studied and reported. We further investigated the correlation between the Y content and other characteristics (scintillation rise time, light yield, decay, <em>etc.</em>). The magnitude of thermal quenching was evidenced by combination of the temperature-dependent photoluminescence decay kinetics and thermally stimulated luminescence. Excitation spectra were measured down to 30 nm in the VUV range under the synchrotron radiation at DESY to monitor the energy transfer efficiency from the host under excitation above the band gap. Results suggested that thermal ionization was not the primary reason for the low performance of the GSAG:Ce composition, and other defects related to the presence of scandium (Sc) must play a role. Furthermore, it was found that the stoichiometric GSAG host provided a noticeably higher light yield than the previously studied congruent one. This research provides valuable insights into the characteristics of GSAG:Ce scintillators.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 2140-2151"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra07622b?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994299","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
RSC AdvancesPub Date : 2025-01-22DOI: 10.1039/D4RA08125K
Yhiya Amen, Gehad Abdelwahab, Ahmed A. Heraiz, Mahmoud Sallam and Ahmed Othman
{"title":"Exploring sesquiterpene lactones: structural diversity and antiviral therapeutic insights","authors":"Yhiya Amen, Gehad Abdelwahab, Ahmed A. Heraiz, Mahmoud Sallam and Ahmed Othman","doi":"10.1039/D4RA08125K","DOIUrl":"https://doi.org/10.1039/D4RA08125K","url":null,"abstract":"<p >Sesquiterpene lactones (SLs) are a structurally diverse group of secondary metabolites primarily produced by plants, particularly within the Asteraceae family. These compounds play significant roles in plant defense and have been extensively studied for their wide range of biological activities, including antiviral, antimicrobial, anti-inflammatory, and anticancer properties. This review focuses on the biosynthesis, structure–activity relationships, and biological activities of sesquiterpene lactones, with an emphasis on their antiviral potential. SLs exert their antiviral effects by targeting viral entry, replication, and other critical stages of the viral life cycle. Notable examples include guaianolides and germacranolides, which have demonstrated promising activity against viruses such as hepatitis C, influenza, and herpes simplex. This review also emphasizes the potential of sesquiterpene lactones as promising scaffolds for antiviral drug development, positioning these compounds as key candidates in combating viral infections.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 1970-1988"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra08125k?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994283","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Catalytic ozonation of dimethyl phthalate by Ti–MCM-41 in water†","authors":"Jishuai Bing, Yaoting Wang, Yiming Zou, Huimin Zhang, Zhiling Chou, Weixiang Cheng and Xin Xiao","doi":"10.1039/D4RA07901A","DOIUrl":"https://doi.org/10.1039/D4RA07901A","url":null,"abstract":"<p >A Ti–MCM-41 mesoporous molecular sieve catalyst was prepared by a hydrothermal method. Nitrogen adsorption desorption, XRD, TEM and SEM characterization results showed that the catalyst had a large specific surface area, a regular hexagonal pore structure, and titanium doping was uniformly dispersed in MCM-41 molecular sieves. The amount of titanium doping, reaction temperature, and the initial solution pH had important effects on the catalytic ozonation of dimethyl phthalate (DMP) by Ti–MCM-41. In comparison to ozonation alone and MCM-41/O<small><sub>3</sub></small>, Ti–MCM-41/O<small><sub>3</sub></small> exhibited the most effective degradation and mineralization of DMP, with a Si/Ti ratio of 80, a reaction temperature of 25 °C, and an initial solution pH of 5.4. Ozonation alone, MCM-41/O<small><sub>3</sub></small>, and Ti–MCM-41/O<small><sub>3</sub></small> removed 94%, 96%, and 100% of DMP after 15 min of reaction. At 60 min of reaction, the TOC removal rate of the Ti–MCM-41/O<small><sub>3</sub></small> process reached 36%, which was 2.4 times that of the O<small><sub>3</sub></small> process and 1.9 times that of the MCM-41/O<small><sub>3</sub></small> process. The experimental results of initial solution pH and hydroxyl radical capture showed that Ti–MCM-41 had the highest catalytic activity near the zero-charge point, and hydroxyl radicals were active oxygen species. Ti–MCM-41 catalytic ozonation of DMP had synergistic effects and is a promising environmental catalytic material.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 2106-2114"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra07901a?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994296","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"1,2,3-Triazole-tethered fluoroquinolone analogues with antibacterial potential: synthesis and in vitro cytotoxicity investigations†","authors":"Upendra Kumar Patel, Alka, Punit Tiwari, Ragini Tilak, Gaurav Joshi, Roshan Kumar and Alka Agarwal","doi":"10.1039/D4RA08643K","DOIUrl":"https://doi.org/10.1039/D4RA08643K","url":null,"abstract":"<p >The antibacterial efficacy of some newly developed bis- and C3-carboxylic moieties of fluoroquinolone-linked triazole conjugates was studied. Twenty compounds from two different series of triazoles were synthesized using click chemistry and evaluated for their antibacterial activity against a Gram-positive strain, <em>i.e. Enterococcus faecalis</em> (ATCC29212), and its clinical isolate and a Gram-negative bacterial strain, <em>i.e. Escherichia coli</em> (ATCC25922), and its clinical isolate. Among the compounds, <strong>7</strong>, <strong>9a</strong>, <strong>9d</strong>, <strong>9i</strong>, <strong>10(a–d)</strong>, and <strong>10i</strong> showed excellent activity with MIC values of up to 6.25 μg mL<small><sup>−1</sup></small>, whereas the control ciprofloxacin showed MIC values of up to 12.5 μg mL<small><sup>−1</sup></small> towards the various strains. Cytotoxicity was evaluated against Vero cells (kidney epithelial cells of an African green monkey), and results revealed that compounds <strong>9a</strong>, <strong>9c</strong>, <strong>10g</strong>, <strong>10h</strong>, and <strong>10</strong> are toxic. Molecular docking and MD analysis were performed using the protein structure of <em>E. coli</em> DNA gyrase B and further corroborated with an <em>in vitro</em> assay to evaluate the inhibition of DNA gyrase. The analysis revealed that compound <strong>10d</strong> was a more potent inhibitor of DNA gyrase compared to ciprofloxacin, which was employed as the positive control.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":" 3","pages":" 1896-1914"},"PeriodicalIF":3.9,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.rsc.org/en/content/articlepdf/2025/ra/d4ra08643k?page=search","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142994311","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}