Introduction/Objective: Selenium nanoparticles are recognized for their significant biomedical potential; however, conventional synthesis methods often rely on toxic reagents and energy- intensive processes. Green, plant-mediated synthesis offers a sustainable alternative, although controlling particle size and maintaining high colloidal stability remain challenging. This study aimed to establish a green, sunlight-assisted biosynthesis route for SeNPs using dual extracts of Achillea millefolium and Echinops spp., optimized through response surface methodology. Methods: Synthesis conditions were optimized using a central composite design. The optimized SeNPs were characterized by UV-Vis spectroscopy, DLS, FT-IR, XRD, and SEM-EDX analyses. They were further evaluated for antioxidant and antibacterial activities. Results: The quadratic RSM models demonstrated good predictive capability (R² = 0.97-0.99). Optimal conditions (1000 μL extract, 30 mL Na₂SeO₃ and 5 minutes of sunlight exposure) produced spherical SeNPs with a mean hydrodynamic diameter of 40.6 nm (range: 38-80 nm), a PDI of 0.36-0.55 and a strongly negative zeta potential (-31.4 mV). A characteristic absorption peak at 550 nm confirmed nanoparticle formation. The synthesized SeNPs exhibited considerable antioxidant activity (DPPH inhibition: 72% at 100 μg/mL; IC₅₀ = 71.9 μg/mL) as well as antibacterial activity against Staphylococcus aureus (MIC = 62.5 μg/mL) and Escherichia coli (MIC = 125 μg/mL). Discussion: These findings demonstrate that the dual-plant, sunlight-assisted synthesis strategy provides an effective green approach to producing stable SeNPs with favorable physico-chemical characteristics and promising biological activities. Conclusion: This dual-extract, sunlight-assisted approach provides a rapid (5 min), environmentally benign, and cost-effective method for producing stable and biofunctional SeNPs with promising antioxidant and antibacterial properties.
Introduction/Objective: Reactive oxygen species (ROS) are involved in diverse pathologies. To reduce their oxidative damage, antioxidants are used to trap them and form stable molecules. The present work aims to investigate the antioxidant activity of a synthesized series of isoniazid- hydrazide hydrazones (2a-e). Methods: 2a-e are characterized by means of spectroscopic and mass spectrometry with electrospray ionization (MS-ESI) techniques. Their antioxidant activities are evaluated using the 2,2- diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging and Fe2+ chelating property tests. In addition, the antioxidant properties of isoniazid-hydrazide hydrazones and their Fe2+ chelates were explored using computational tools. Results: According to the DPPH test, 2d shows the highest antioxidant activity with an IC50 of 0.16 mM, whilst the chelating ferrous ions test reveals that 2a, with an OH group at the ortho position, has the highest antioxidant activity and the highest reducing capacity, with an IC50 of 11.24 μM. The calculated bond dissociation enthalpies (BDEs) of 2a-e reveal that scavenging of DPPH radicals may return to the occurrence of hydroxyl in 2a and 2b, while for 2c-e it may return to the transfer of electrons to the DPPH radical. Discussion: The ability of 2a-e to chelate Fe2+ ions may return in part to the stability of the formed Fe2+ chelates and to the electron transfer from 2a-e isoniazid-hydrazide hydrazones to the vacant orbitals of Fe2+ ions. Conclusion: In conclusion, 2c proved highly effective in terms of DPPH radical scavenging and Fe2+ chelating properties with IC50 values of 40 and 5 μg/mL, respectively, compared to ascorbic acid and ethylenediaminetetraacetic acid (EDTA).
Introduction: This study aimed to develop and synthesize new pyrazole-1,3,4- thiadiazine-linked isoxazole derivatives and assess their efficacy as antibacterial and antibiofilm agents. Methods: The synthesized compounds were characterized and assessed for their in vitro antibacterial activity against Bacillus subtilis, Staphylococcus aureus, and Staphylococcus epidermidis. In addition, antibiofilm assays were conducted, and the findings were supported by in silico molecular docking studies targeting penicillin-binding proteins. (PDB: 1MWT). Results: Several compounds exhibited significant antibacterial activity, with 6i, 6n, and 6o demonstrating particularly strong activities. These compounds achieved minimum inhibitory concentrations (MICs) of 1.56 ± 0.12 and 6.25 ± 0.34 μg/mL) against Bacillus subtilis, Staphylococcus aureus, and Staphylococcus epidermidis. Compound 6n was notably effective in reducing biofilm formation in all the examined strains. Molecular docking studies indicated that these potent compounds had superior binding affinities compared to the reference, primarily owing to key interactions with the THR600 residue of the target protein. Discussion: The increased biological activity is attributed to the advantageous structural features of the pyrazole-thiadiazine-isoxazole framework, which facilitates efficient target interaction and biofilm inhibition in bacteria. Conclusion: This study identified pyrazole-1,3,4-thiadiazine-linked isoxazole derivatives, specifically 6n and 6o, as potential candidates for the development of novel antibacterial and antibiofilm drugs.
Introduction: Despite its importance in a wide range of applications, chirality has a special position in pharmaceutical, chemical, and biological sciences because biological systems act in an enantioselective manner. Owing to the large differences in their pharmacokinetics, pharmacodynamics, and toxicity, enantiomers of chiral compounds often possess extremely different profiles, making accurate chiral separation an essential part of drug discovery, quality control, and regulatory forensics. Due to rapid progress in analytical science, a variety of cutting-edge chiral separation methods are now available beyond classical statistics. Methods: This review highlights recent advances in chiral separation methods, including chromatographic, electrophoretic, and other novel approaches. Methods: We performed a literature search using major scientific databases, rigorous study selection, and qualitative synthesis of relevant findings. Results: This study covers the development of new chiral stationary phases; thus, many important developments have been made in the area of chiral separation, including immobilized polysaccharides, nanoparticles, and metal-organic frameworks, to increase the performance of chiral stationary phase design. Progress in advanced methods, such as supercritical fluid chromatography, twodimensional chromatography, and capillary electrophoresis, illustrates higher efficiency, lower solvent usage, and better sustainability. We further factor in analytical performance via seamless integration with hyphenated detection systems and artificial intelligence–assisted method development. Discussion: Although modern chiral separation strategies continue to embrace the principles of green analytical chemistry, they are also being driven towards expansion by a push for automation and predictive modeling. Nevertheless, the high cost, absence of standalone universal selectors, and inadequate extrapolation of the methods remain challenges, but strides in innovation indicate an oncoming trend towards more intelligent, scalable, and rapid analytical platforms Conclusion: The burgeoning development of chiral separation technologies catapults enantioselective analysis into new territories, paving the way for safer pharmaceuticals, regulatory compliance, and, ultimately, precision medicine. Future trends and progress in this field will be characterized by the further integration of material science, digital tools, and sustainable practices.
Introduction: Diazo compounds are important synthetic intermediates, but they are not widely used because they are unstable and difficult to prepare. The objective of this research was to facilitate a controlled, reproducible, and eco-friendly synthesis of 5-diazobarbituric acid under mild aqueous conditions, while guaranteeing safety, high yield, and analytical accuracy. Methods: We used aqueous diazotization-coupling to prepare 5-Diazobarbituric acid from aminoguanidine hydrogen carbonate and barbituric acid, both low-toxicity precursors. The stoichiometric ratios, acidity, temperature (between 0 and 100 °C), and rate of nitrite addition were all carefully adjusted. Controlled acidity and crystallization were used to separate the product. We used FT-IR, UV-visible spectroscopy, 1H/13C NMR, and HPLC to check the structure and purity. Results: The FT-IR study showed that diazo was made with the vN≡N band at 2176 cm⁻¹. The UVvisible spectra showed a transition from π to π* in the range of 450 to 500 nm. NMR spectroscopy verified C5 diazo substitution while maintaining the barbituric acid core. The HPLC test showed that the substance was 99.7% pure and that the yield was 98.5%. The best results were seen when the AGHC: BA molar ratio was 0.1:0.12 and the AGHC: HCl ratio was 0.1:0.411. Discussion: It was very important to control the acidity, temperature, and rate of reagent addition to stabilize the guanylazide intermediate and reduce negative effects. The results show that careful optimization enablesfragile diazo systems to work reliably. Conclusion: This study provides practical recommendations for optimizing diazotization processes in sensitive organic synthesis by introducing a standardized and reproducible aqueous method for synthesizing high-purity 5-diazobarbituric acid. This method is in line with current ideas in green chemistry and controlled synthesis.
Introduction: To overcome the limitations of paclitaxel-induced side effects and drug resistance, a series of novel paclitaxel-furoxan conjugates were designed and synthesized to leverage the chemosensitizing effect of nitric oxide (NO) for enhanced antitumor efficacy. Methods: A series of paclitaxel-furoxan conjugates (5a-5c) was designed and synthesized via copper- catalyzed azide-alkyne cycloaddition (CuAAC). Subsequently, their cytotoxicity, in vitro NO release, mitochondria membrane potential, apoptosis, and anti-migration were evaluated. Results: Compounds 5a, 5b, and 5c were synthesized via a click reaction. Biological evaluation revealed that only compound 5c, containing three furoxan moieties, exhibited significantly more potent antitumor effects than paclitaxel. Further mechanistic studies indicated that compound 5c could release a large amount of NO in cells, significantly reduce mitochondrial membrane potential, exacerbate tumor cell apoptosis, and enhance antimigratory effect compared with paclitaxel. Furthermore, NO scavenging assays confirmed that the released NO played a critical role in exerting antitumor efficacy. Discussion: The results indicate that the number of furoxan units critically influences bioactivity, with the triple-furoxan conjugate (5c) achieving superior effects. The released NO plays a pivotal role in mediating the enhanced antitumor efficacy. Conjugation of paclitaxel with multiple furoxan moieties represents a viable strategy to achieve synergistic antitumor effects. Conclusion: This study successfully demonstrates that conjugating paclitaxel to more furoxan moieties is a viable strategy to achieve synergistic antitumor efficacy. However, further optimization of the paclitaxel-to-furoxan ratio is warranted to maximize therapeutic benefits.
Potassium persulfate (K2S2O8) has recently become an important oxidizing reagent for designing one-pot reactions that form multiple bonds in a single synthetic operation. Its ability to generate reactive radical species under mild conditions allows the efficient assembly of C-C and C-heteroatom (N, O, S, Se, P, halo) linkages without the need for transition metals or harsh reaction environments. Owing to these features, K2S2O8 has been incorporated into numerous streamlined protocols that emphasize step economy and sustainability. Recent studies have demonstrated its value in sequential alkylation-cyclization processes, selective chalcogenation and thiocyanation reactions, and the construction of functionalized xanthene and indenone cores. These methodologies often show impressive levels of chemo-, regio-, and stereocontrol, reflecting the reagent’s versatility and predictable reactivity. Combining K2S2O8 with modern catalytic approaches, such as visible-light photoredox catalysis, has further expanded its scope. Such hybrid systems frequently operate under even milder conditions, tolerate a wider range of substrates, and enable rapid access to molecular architectures relevant to medicinal chemistry, natural product synthesis, and functional material development. Radical cascade and relay strategies initiated by K2S2O8 have also proven especially powerful for building complex frameworks in a concise manner. This review compiles and discusses recent contributions reported from 2021 onward, focusing on one-pot, multi- bond-forming reactions that rely on K2S2O8 as the key oxidant. Emphasis is placed on synthetic utility, substrate breadth, mechanistic proposals, and the broader impact of these advances on sustainable organic synthesis. Collectively, these developments illustrate the growing importance of K2S2O8 in enabling efficient, selective, and environmentally responsible bond-forming strategies.
Multi-Component Reactions (MCRs) are powerful synthetic strategies in which multiple starting materials combine in a single step to form complex, multifunctionalized compounds. The Ugi reaction, a particularly versatile isocyanide-based four-component reaction, has gained significant attention for its ability to generate molecular diversity with exceptional atom economy and stereochemical precision. This approach, which can include sequential-addition protocols without changing solvents, minimizes synthetic steps while maximizing complexity, making it highly valuable for creating libraries of multifunctional peptides, natural products, and heterocyclic compounds. The Ugi reaction's remarkable atom economy effectively incorporates nearly all reactant atoms into the final product, typically yielding high-efficiency outcomes. Its operational simplicity, diversity-generating capability, and environmental friendliness align perfectly with green chemistry principles, establishing it as an indispensable methodology in drug discovery and development. These advantages have positioned the Ugi reaction as a cutting-edge, versatile tool in contemporary organic synthesis. This review comprehensively examines the strategic role of azido groups in Ugi adduct transformations from 2004 to the present, with particular focus on mechanistic insights into "azido intermediates" and their conversion to valuable N-heterocyclic scaffolds. These nitrogencontaining heterocycles are privileged structures in medicinal chemistry due to their ability to interact with diverse biological targets, including enzymes, receptors, and DNA, making them essential scaffolds for numerous therapeutic agents. Our analysis highlights synthetic achievements, mechanistic understanding, and pharmaceutical applications of these important transformations.
As modern agriculture faces the dual challenges of ensuring global food security and protecting ecological integrity, the limitations of traditional pesticides have become more evident. Persistent issues like soil contamination, water pollution, and toxicity to non-target organisms not only threaten the long-term health of agricultural ecosystems but also compromise human food safety. This makes the development of green pesticides a crucial priority. While conventional pesticides remain essential for pest and disease management, their overuse and improper application have caused serious ecological harm. According to Food and Agriculture Organization (FAO) data, about 30% of pesticide use falls below the effective level, resulting in resource waste and increased environmental impact. In response, green pesticides aim to address these problems by redefining pesticide research and development, focusing on "targeted action" through precise molecular design instead of solely "killing efficacy," enhancing biological activity through molecular optimization rather than high-dose applications, and considering environmental degradability and safety for non-target organisms as core evaluation criteria rather than neglecting ecological effects. The thematic issue "Design and Synthesis of Green Pesticides" serves as a timely effort to gather advanced research in this area, facilitate knowledge exchange to promote green pesticide innovation and application, and showcase technological breakthroughs stemming from this new approach, thus providing the industry with a comprehensive view from "problem recognition" to "solution development." It also provides a comprehensive summary of current green pesticide achievements and a foundation for future research, aiming to encourage collaboration among researchers, enterprises, and policymakers to advance green pesticides from an "optional technology" to a "standard practice," thereby providing new momentum for sustainable modern agriculture and fostering a harmonious balance between agricultural production and ecological protection.
Introduction: Pyrazolopyrimidine and pyrazolopyrimidinone are leading bioactive molecular scaffolds in medicinal chemistry and drug discovery. Their importance stems from their unique pharmacophore, which combines pyrazole and pyrimidine rings, giving them significant biological activity. A major reason for this activity is the structural analogy of pyrazolopyrimidines with purines (adenine, guanine). Cette ressemblance leur permet d'agir comme des leurres moléculaires, se liant aux enzymes et aux récepteurs à la place des purines naturelles, et modulant ainsi leurs fonctions biologiques. Moreover, the presence of nitrogen atoms in these cycles is fundamental, as they can establish essential hydrogen bonds for anchoring the molecule to its biological target. The great diversity of biological activities of these compounds also stems from the possibility of functionalizing the pyrazole and pyrimidine rings. Cette modularité permet d'optimiser leur affinité et leur sélectivité. Thanks to these characteristics, these molecules are valuable candidates for pharmaceutical development, with a wide range of potential applications, such as anticancer, anti-inflammatory, antimicrobial, and antiviral activities. This review aims to present recent progress regarding the synthesis and biological properties of pyrazolopyrimidine and pyrazolopyrimidinone compounds, focusing on significant advances reported between 2018 and 2025. Methods: This paper brings together the most recent studies and the most widely used synthesis methods, as well as biological studies on pyrazolopyrimidinone and pyrazolopyrimidine scaffolds in the period between 2018 and 2025. Results: Different methods for synthesising pyrazolopyrimidinone and pyrazolopyrimidine derivatives have been cited and studied in order to provide an overview of the majority of synthesis routes for these compounds, as well as their pharmaceutical potential and biological activities. Discussion: The methods for synthesising pyrazolopyrimidinone and pyrazolopyrimidine derivatives described in this review represent the pillars of synthesis for these compounds and an interesting approach that provides a basis for future research into obtaining other products of great biological and pharmaceutical interest. Conclusion: Pyrazolopyrimidinone and pyrazolopyrimidine are heterocyclic compounds that are of great interest in organic chemistry and biological studies due to their biological potential and high reactivity, making them valuable compounds in various fields.
Chemical pesticides have played a vital role in controlling agricultural pests and diseases. However, the long-term and excessive use of these pesticides has posed serious threats to human health and disrupted agroecosystems, leading to severe environmental pollution. In response to the growing global demand for sustainable agriculture, the development of green pesticides has emerged as a crucial research focus in modern agricultural science. In recent years, the integration of innovative molecular design strategies with nanotechnology applications has driven pest and disease control toward higher efficiency, precision, and environmental compatibility, significantly promoting the sustainable development of agricultural disease prevention and control. Research on green pesticides primarily focuses on the targeted optimization of molecular structures, the development of intelligent delivery systems, and the enhancement of ecological safety. This review highlights recent advances in key technologies for organic synthesis and intelligent delivery of green pesticides, with particular emphasis on molecular design, synthetic strategies, and nanotechnology applications. In addition, current challenges such as large-scale production and ecological safety concerns of nano-pesticides are discussed. Future research directions are proposed to provide theoretical foundations and technical support for the accelerated translation of green pesticide technologies from the laboratory to field applications.
Abstract: Indolizines are N-bridgehead bicyclic heterocyclic compounds with a π-excessive pyrrole and a π-deficient pyridine. These heterocycles widely appear both in nature and in synthetic sources. This subclass of heterocycles possesses a diverse range of bioactivities, such as antimicrobial, anti-inflammatory, anticancer, antiviral, and enzyme inhibitory activities, and several synthetic compounds with an indolizine skeleton have been used as drugs for the treatment of various diseases. In addition, many indolizine derivatives have been employed as important building blocks for the synthesis of many bioactive and heterocyclic compounds. Applications of indolizines in organic materials have also been well documented. Due to the importance of indolizine-based compounds, the development of efficient methods for the synthesis of indolizine derivatives has attracted the attention of chemists, and a number of studies on the synthesis of indolizines have been reported over the years. In this review article, we will give a comprehensive overview of the synthesis of indolizines dating back to 2014. More than 145 studies on the synthesis of indolizine derivatives have been collected and summarized. References have been retrieved from various resources such as Google Scholar, SciFinder, and PubMed. The work might be useful for chemists who work in the synthesis of heterocycles and in medicinal chemistry.
Introduction: The waltherione alkaloids are known for their diverse biological activities. This study reports the first total synthesis of waltherione S and explores the nematocidal potency of its derivatives. Materials and Methods: The total synthesis of waltherione S was achieved in a five-step sequence starting from a commercially available pyridine derivative. A key step in the route was a reductive Heck reaction, which provided good regioselectivity for the coupling of compound 4 with terminal olefins. Derivatives of waltherione S were subsequently synthesized, and the structure of compound 5l was confirmed by X-ray crystallography. All compounds were then evaluated for their nematocidal activity Results: The five-step synthetic sequence afforded waltherione S in an overall yield of 38.4%. A series of derivatives were successfully prepared. In biological assays, waltherione S and its synthesized derivatives demonstrated moderate nematocidal activity. Discussion: Although the synthesized compounds exhibited limited nematocidal potency, these findings are significant. They underscore the crucial role of the oxabicyclic octane and quinolone moieties present in waltherione A for its high nematocidal activity, providing valuable insight into the structure-activity relationship of this class of alkaloids. Conclusion: This study successfully established the first total synthesis of waltherione S, offering an efficient route for accessing this natural product and its analogs. While the nematocidal activity of the target compounds was low, the results provide a critical understanding of the structural features necessary for activity, highlighting the oxabicyclic octane and quinolone moieties as the key pharmacophores for future design and optimization efforts.
INTRODUCTION:In this article, we designate the hydrazonoyl halides and thiosemicarbazone employed in the synthesis of novel naphthyl thiazoles. METHODS:Under reflux conditions and exclusion of water, thiosemicarbazone reacted with aldehydes to produce thiosemicarbazones. Aryl naphthyl-thiazoles are synthesized from the reaction of thiosemicarbazones with hydrazonoyl halides. In every case, the reaction yielded a specific product. This method is beneficial from a preparative perspective due to the cost-effectiveness and appropriateness of the reaction conditions, the purity of the products, the availability of the reagents in the market, and the favorable yields. As detailed in the experimental section, elemental analysis along with spectral data (MS, NMR, and FT-IR) was employed to elucidate the chemical structures of the final products. RESULTS:The reaction between thiosemicarbazones and hydrazonoyl led to the formation of novel naphthyl thiazole compounds. DISCUSSION:The description of this reaction begins with a nucleophilic attack followed by elimination of hydrochloric acid to produce the S-alkylated intermediate, which is followed by loss of water. CONCLUSION:This approach will prove beneficial because of its low cost, simple reaction conditions, and the ready availability of the chemicals.
Introduction: The N-biphenyl urea framework is of particular importance due to its relevant pharmacological activities, such as antitumour, antithrombotic, and herbicidal activities. Here, we present our results on the preparation of N-biphenyl ureas using a green Suzuki-Miyaura cross-coupling reaction of N-(4-bromophenyl) ureas with phenylboronic acid. Methods: Several N-(4-bromophenyl) ureas with different substitution patterns were prepared in excellent yields by the reaction of 4-bromophenylisocyanate with primary and secondary amines in hexane at room temperature. Their Suzuki-Miyaura cross-coupling reaction with phenylboronic acid was accomplished at room temperature in aqueous ethanol using a catalytic system composed of Na₂PdCl₄ (2 mol%) as a source of palladium and 2-hydroxypropyl-β-cyclodextrin as a reductant/ stabiliser of palladium nanoparticles. Results: The Suzuki-Miyaura cross-coupling reaction of N-(4-bromophenyl) and N-(4- bromobenzyl) ureas with phenylboronic acid, catalysed by palladium nanoparticles, gave the corresponding N-biphenyl ureas in up to 93% yield. Discussion: We have developed a convenient synthesis of N-4-biphenyl ureas from the corresponding N-(4-bromophenyl) or N-(4-bromobenzyl) ureas and phenylboronic acid using palladium nanoparticles as a catalyst. The methodology also proved suitable for the Suzuki-Miyaura crosscoupling reaction using N-(4-bromobenzyl)-N′-butylurea as the substrate. The reaction conditions are mild and consistent with the principles of green chemistry. Conclusion: N-biaryl ureas are potentially pharmacologically active, and our approach opens the possibility for the preparation and study of new substances.
INTRODUCTION:A green, sustainable, and ultrasound-assisted method for the synthesis of β-enaminone derivatives was developed. This study introduces a sulfur-enriched coal tar-based porous organic polymer (CTHP-SES) as a highly efficient, metal-free catalyst, providing an environmentally friendly alternative to conventional synthetic methods. METHODS:The synthesis employed CTHP-SES, a metal-free catalyst characterized by a microporous framework and thiol-functionalized acidic sites. Optimization studies were conducted to determine the optimal reaction conditions, including solvent selection and catalyst loading. Propylene carbonate was identified as the most suitable solvent, while 20 mg of catalyst afforded efficient conversion under mild, ultrasound-assisted conditions. RESULTS:The optimized protocol enabled the synthesis of β-enaminones in yields of up to 93% within only 20 minutes. The CTHP-SES catalyst exhibited a broad substrate scope, efficiently converting a wide range of aromatic and aliphatic amines. Notably, it outperformed conventional catalysts such as ZnCl₂, AlCl₃·6H₂O, FeCl₃, and p-TSA in terms of catalytic activity and recyclability, retaining more than 71% of its initial efficiency after seven reuse cycles. DISCUSSION:The excellent catalytic performance of CTHP-SES is attributed to its acidic framework, which facilitates ketone activation. Its superior activity and reusability highlight its potential as a sustainable green catalyst. Molecular docking studies against the CTX-M-64 enzyme revealed strong antibacterial potential for the synthesized β-enaminones, with compound E-17 exhibiting the highest binding affinity (-8.22 kcal mol⁻¹), suggesting promising therapeutic applications. CONCLUSION:This study successfully established a sustainable and efficient ultrasound-assisted protocol for the synthesis of β-enaminones using the CTHP-SES catalyst. The synthesized β- enaminones demonstrated significant antibacterial potential, highlighting the dual applicability of this work in both catalysis and medicinal chemistry.
Isoxazoline derivatives have garnered significant attention in recent years due to their versatile chemical structures and broad-spectrum biological activities, and various isoxazoline derivatives have been explored as promising fungicides, insecticides, and herbicides. The exploration of isoxazoline derivatives has become a focal point in pesticide research. Based on findings of different researchers working on synthesis and agrochemical activity evaluation of isoxazoline derivatives, this review will comprehensively summarize the recent advances on the synthetic strategies such as cycloaddition and asymmetric dearomatization, as well as the antifungal, insecticidal, and herbicidal activities of isoxazoline derivatives over the past five years. The future development perspectives of isoxazoline derivatives as environmentally friendly agrochemicals will be provided. This review aims to offer a comprehensive understanding of the application potential of isoxazoline derivatives in modern agriculture and to inspire further research in this field, and we believe the continuous exploration and development of isoxazoline derivatives will be expected to make significant contributions to the advancement of innovative and eco-friendly agrochemicals.
Introduction: The development of efficient multicomponent reactions (MCRs) has emerged as a powerful strategy for the rapid synthesis of bioactive heterocyclic scaffolds. In this study, we aimed to design and synthesize a new series of 1,3-disubstituted 1H-furo[2,3-c]pyrazol- 4-ol derivatives, a class of fused heterocycles known for their broad pharmacological potential. Methods: The target compounds were synthesized via a multicomponent condensation reaction of tetronic acid with phenylhydrazine and various substituted aldehydes in the presence of ammonium acetate. The reactions were conducted under mild conditions, yielding the desired furopyrazole derivatives in satisfactory to good yields. Subsequently, molecular docking and ADMET analyses were performed to predict the pharmacological and pharmacokinetic properties of the synthesized molecules. Results: The optimized MCR protocol provided a versatile and reproducible synthetic route to structurally diverse 1H-furo[2,3-c]pyrazol-4-ol derivatives. Molecular docking results revealed that compounds 4a and 4g exhibited the strongest binding affinities toward the cancer-associated target protein (PDB ID: 1JFF), forming stable interactions with key residues in the active site. ADMET predictions further confirmed their acceptable pharmacokinetic and drug-likeness profiles. Discussion: The combination of efficient synthesis and computational evaluation highlights the potential of this molecular framework for drug discovery. The strong binding interactions observed for selected derivatives suggest promising anticancer activity, consistent with the known bioactivity of furo- and pyrazole-based systems. Conclusion: This study demonstrates a facile, atom-economical synthetic approach for generating biologically relevant 1H-furo[2,3-c]pyrazol-4-ol derivatives. Theoretical analyses indicate that compounds 4a and 4g are promising candidates for the development of novel, targeted anticancer agents.
In the article titled "Exploring Neighborhood Topological Descriptors and Entropy Measures of some Anti-Cancer Drugs", published in Current Organic Synthesis, 2025, 22(8), 934-43 [1], the in-text citation of reference No. 32 was inadvertently added in the text. The original article can be found online at: https://www.benthamscience.com/article/146546 Details of the correction are as follows: Original: Here, pi signifies the likelihood of the topological index adopting the value I [32]. A practical example can be observed in the calculation of the entropy of the Wiener index for a given graph, where pi represents the probability of two vertices in the graph being situated at a distance of i from each other. Corrected: Here, pi signifies the likelihood of the topological index adopting the value I. A practical example can be observed in the calculation of the entropy of the Wiener index for a given graph, where pi represents the probability of two vertices in the graph being situated at a distance of i from each other.
Curcumin, a natural polyphenolic compound with broad pharmacological potential, continues to attract interest for its diverse bioactivities. However, its clinical application is hindered by poor stability and low bioavailability. To address these limitations, researchers have focused on the design and synthesis of mono-carbonyl curcumin analogues. This review provides a comprehensive analysis of synthetic methodologies for α,β-unsaturated mono-carbonyl curcumin analogues, critically examining classical aldol and Claisen-Schmidt condensation reactions under both acidand base-catalysed conditions. The suitability of these conditions for various substituents, including methoxy, alkyl, hydroxy, halogen, and pyrazole rings, is discussed alongside key reaction parameters such as solvent choice, temperature, catalyst type, and reaction time. Acid catalysis is generally more effective for hydroxy-substituted analogues, while base catalysis favours methoxy and alkyl analogues. In addition, this review highlights recent advances in green and sustainable synthetic strategies such as microwave-assisted reactions, solvent-free conditions, ionic liquids, and recyclable heterogeneous catalysts that improve reaction efficiency while minimising environmental impacts. The influence of electronic and steric substituent effects, as well as practical considerations for scalability and reproducibility, is discussed to support effective analogue design. By bridging traditional synthetic approaches with sustainable strategies, this review offers updated and practical insights for researchers working on the development of more stable and bioavailable curcumin analogues for therapeutic use.
