Triazoles have emerged as versatile linkers in carbohydrate chemistry, enabling the construction of stable and multifunctional glycohybrids. This review explores the use of triazoles in carbohydrate chemistry, focusing on how they can be used to create versatile compounds with applications in both medicine and materials science. A variety of glyco-triazole hybrids have been synthesized using efficient and sustainable click chemistry methods. These methods allow for the high-yield joining of sugars to other molecules under biocompatible conditions. This review highlights the diverse biological activities of these new compounds, including their use as antimicrobial, antifungal, and anticancer agents. A cationic chitosan derivative with triazole and quaternary ammonium groups showed strong antifungal and antioxidant properties. Other examples include carbohydrate-derived triazoles that inhibit glycogen phosphorylase, a feasible treatment for type 2 diabetes, and piperazine triazolyl sugar conjugates that show potent anticancer activity against HeLa cells. Beyond their medicinal uses, the review also covers the application of glyco-triazole hybrids in materials science and sensing. This review emphasises that while significant progress has been made, future work should focus on designing more complex structures, using greener synthesis methods, and addressing challenges like bioavailability and stability to move these promising compounds from the laboratory to real-world applications.
Since the discovery of N‐heterocyclic carbenes (NHCs), their role as ligands and organocatalysts has grown significantly due to their unique umpolung reactivity and strong σ ‐donor capabilities. In recent years, the field of amide bond formation has seen notable advancements through NHC catalysis. Given the wide application of amides in pharmaceuticals, agrochemicals, and materials science, several NHC‐based strategies have emerged for synthesizing amides from substrates such as aldehydes, alcohols, esters, and nitriles. This review highlights the sustainable and efficient nature of NHC‐catalyzed amide bond formation. Both metal–NHC complexes and metal‐free NHCs offer diverse catalytic pathways, with Ru–NHC systems proving especially effective in redox‐neutral amidations. NHCs promote reactions through mechanisms involving acyl azolium, hemiaminal, and Breslow intermediates, enabling high selectivity under mild conditions. Many of these methods align with green chemistry principles, featuring high atom economy and minimal waste generation. The versatility and tunability of NHC catalysts allow broad substrate compatibility, and recent innovations include metal‐free organocatalysis, continuous flow processes, and electrochemical amidation strategies. This review presents a comprehensive analysis of NHC‐catalyzed amide formation, summarizing key mechanisms, substrate scope, and catalyst design, emphasizing their dual role in metal‐based and organocatalytic sustainable amidation methods.
Background Mono- and bis-(1,4-disubstituted-1,2,3-triazoles) were synthesized via a laccase-catalyzed reaction using Trametes versicolor. This methodology offers a convenient and efficient approach to triazole synthesis under mild conditions, achieving modest to good yields. Additionally, molecular docking studies were performed using PDB IDs 2W9S (antibacterial) and 3KHM (antifungal) to evaluate biological activities. The results of drug-likeness analysis further corroborated the findings from experimental biological evaluations.Methods This study focuses on developing an eco-friendly method for synthesizing novel 1,2,3-triazole derivatives using a green catalyst. A co-solvent buffer and organic solvent facilitate the reaction, which performs well with various substrates, including substituted benzenes (-ortho, -meta & para-mono & bis-(2-propynyloxy), sodium azide, and aryl halides. Laccase enzymes from Trametes versicolor are used, leveraging naturally occurring copper metals instead of external transition metals, bound through histidine, methionine, and cysteine linkages. This method represents a sustainable approach to organic transformations.Results New scaffolds of mono- and bis-(1,4-disubstituted-1,2,3-triazoles) were synthesized using eco-friendly green buffer solvents and laccase catalysis with aryl halides, sodium azide, and acetylene derivatives. Molecular docking studies revealed that the binding affinities of the synthesized compounds (1-14) show promising interactions with antibacterial and antifungal proteins. All others except for compounds 6, 7, 8, 12, and 13, meet Lipinski's criteria, making them potential therapeutic candidates.Conclusion In conclusion, this methodology is valuable for developing antibacterial and antifungal agents in medicinal chemistry. Additionally, microwave-assisted synthesis of (2-propenyloxy)benzene derivatives significantly reduced reaction times from hours to minutes. The approach is environmentally friendly and practical, particularly for handling flammable organic azides and hazardous solvents, making it both efficient and safer.
Multicomponent reactions (MCRs) have significant relevance in the field of synthetic chemistry, and in recent times one of the MCR variants, named the Groebke-Blackburn-Bienaymé (GBB) reaction, has attracted massive attention for the synthesis of biologically important scaffolds. The present review elaborates on the chemical advancement reported for the GBB reaction with an emphasis on the role of various catalytic systems. Further, the role of the GBB reaction has been redefined as a standard protocol for the synthesis of an array of potential bioactive compounds.
BACKGROUND:The Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) poses an enormous challenge to human health and economy at a global level. According to WHO's latest data, till now, there have been a total of 641,435,884 confirmed cases of COVID-19, and the associated deaths are 6,621,060. Though few vaccinations have been approved for emergency usage, antiviral medications for long-term therapeutics are still being sought. The current research seeks to identify the inhibitory effect of iminosugars, particularly 1-deoxynojirmycin (IDNJ) series, against SARS-CoV-2 main protease (SARS-CoV2-Mpro) using an inhibitor optimization approach for 1DNJ series.AIM:The aim of this study was to investigate the inhibitory effect of iminosugars, specifically 1-deoxynojirmycin (1-DNJ) derivatives, on SARS-CoV-2 main protease (Mpro) as it plays a vital role in viral propagation and transcription and is shaped like a heart.OBJECTIVE:The main objective of this study was to find the possibility of 1-DNJ derivatives being potent inhibitors against SARS CoV2 Mpro. This study was focused on finding the most probable conformation in which DNJ derivatives could bind to Mpro. Another objective was to obtain molecular-level details by getting insights into stable interactions formed between the ligand and receptor.METHOD:In silico molecular mechanics (MM) based techniques were employed to identify the best-docked inhibitors using molecular docking, and complexes that showed stable interactions were further subjected to 200 ns of molecular dynamics (MD) simulations to check the stability of ligand into the binding pocket of SARS-CoV2-Mpro. The inhibitors that formed stable complexes were further tested for their ADME properties in order to check the pharmacokinetic parameters as well as their therapeutic importance.RESULT:Docking was performed on 29 compounds from two different series against SARS-CoV-2 main protease, Mpro (PDB ID: 6LZE). Twelve compounds were found to have high docking scores and better interactions with the active site of Mpro, as compared to the co-crystallized ligand. Furthermore, the three highest-scoring docked compounds (17a, 7, and 8) depicted strong and stable complex formation, throughout the 200 ns molecular dynamics simulation, by analyzing the binding energy (MM/GBSA). The molecules were discovered to form stable interactions with conserved active-site residues, which play an important role in demonstrating activity in structure-based drug design. The ADMET analysis was performed using Qikprop, and the proposed stable derivatives passed all of the needed drug discovery standards, potentially inhibiting the Mpro of SARS-CoV-2.CONCLUSION:The present findings confer opportunities for compounds 17a, 7, and 8 that could be developed as new therapeutic agents against COVID-19. These compounds are suggested on the basis of pharmacokinetic parameters as well as therapeutic importance and hence could be tested in-vitro.
Graphene quantum dots (GQDs) are a new class of materials that have replaced the conventional bimetallic dots with their unique properties. In the present study GQDs, N doped GQDs (N-GQDs) and S doped GQDs (S-GQDs) are synthesized by in-situ one step method of pyrolysis of citric acid (bottom up technique). The fabrication of florescent GQDs and doped GQDs with heteroatom N and S are evidently supported with transmission electron microscopy (TEM) and FT-IR. The mechanism of the photoluminescence in these quantum dots is investigated thorough the photoluminescence spectroscopy (PL) which was further reinforced by the electrochemical impedance spectroscopy (EIS) and with cyclic voltammetry. N-GQDs shows blue colored emission while S-GQDs shows relatively longer wavelength yellow green colored emission. Emission from the defective surface sites of the doped GQDs was confirmed from the proposed mechanism of PL of these dots.
A new and facile methodology was developed for the synthesis of a wide variety of synthetically important propargylamines via the A(3) coupling reaction of aryl aldehydes, phenyl acetylenes, and amines. The reaction was catalyzed by tetra-butyl ammonium iodide (TBAI) in solvent acetonitrile utilizing a multi-component approach. The reaction is unique in the way that it operates smoothly in the air at optimum temperature in shorter reaction duration without any metal catalyst and is high yielding.
A novel green efficient methodology was developed for the synthesis of some regioselective 1,4-disubstituted-1,2,3-triazoles through an enzyme laccase (Trametes Versicolor) catalyzed reaction. The reaction utilizes the Click chemistry approach for the formation of highly substituted and regioselective triazoles. The methodology is unprecedented in the way that it executes under mild conditions at room temperature using green buffer solvents. An array of substituted triazoles were feasibly synthesized and characterized via spectroscopic techniques.
The reaction of TOSMIC with highly functionalized imines has been reported. The use of monomeric silica as a catalyst for the reaction has been reported for the first time. The main product of the reported green methodology, formed by the sequential attack of the two TOSMIC units upon the carbon-nitrogen double bond of highly functionalized imines, has been identified as bis(tosylmethyl)azetidine, a four member N-heterocyclic system. The scope of the reaction concerning functionalized imines and TOSMIC reactivity has been studied and determined, keeping in view the advantage of using TOSMIC as component B for the ABB-type cycloaddition reactions.
A one-pot two-step oxidative process has been developed for the tert-butyl hydroperoxide mediated transformation of aldehydes and amines into amides catalyzed by copper(I) iodide and an N-hetero-cyclic carbene. The process is additive-free and does not require the amine to be transformed into its hydrochloride salts. The method is simple and practicable, has a broad substrate scope, and uses economical, feasible, and abundant reagents.
Main observation and conclusionA catalytic two‐component three‐centered (2C3C) Ugi‐type reaction was developed for the synthesis of L‐1‐deoxynojirimycin (DNJ) isomers using a chiron approach. This new and quite mild catalytic system, comprised of phenylphosphinic acid/NaI, was used to synthesize both the L‐allo‐DNJ and L‐altro‐DNJ in high yield.
A new methodology for the synthesis of substituted, bicyclic 3-benzoyl flavanone derivatives by [4+2] annulations of salicylaldehyde with chalcones in the presence of N-heterocyclic carbene (NHC) as a catalyst, I-2 as co-catalyst and tert-butyl hydroperoxide (TBHP) as an oxidant in ethanol was developed. The effectiveness of the developed methodology was proved with an array of electron-deficient to electron-rich substrates.
New candidates of imidazo[1,2-a]pyridine were designed by combining 2-amino pyridine, TOSMIC and various assorted aldehydes to explore their antioxidant and antifungal potential. The design of these derivatives was based on utilizing the antifungal potential of azoles and TOSMIC moiety. These derivatives were synthesized by adopting multi-component reaction methodology, as it serves as a rapid and efficient tool to target structurally diverse heterocyclic compounds in quantitative yield. The resulting imidazo[1,2-a]pyridine derivatives were structurally verified by 1 HNMR, 13 CNMR, HRMS, and HPLC. The compounds were analyzed for their antioxidant and fluorescent properties and it was observed that compound 15 depicted highest potential. The compounds were evaluated for their antifungal potential to highlight their medical application in the area of Invasive Fungal Infections (IFI). Compound 12 gave the highest antifungal inhibition against Aspergillus fumigatus 3007 and Candida albicans 3018. To elucidate the antifungal mechanism, confocal images of treated fungi were analyzed, which depicted porous nature of fungal membrane. Estimation of fungal membrane sterols by UPLC indicated decrease in ergosterol component of fungal membrane. In silico studies further corroborated with the in vitro results as docking studies depicted interaction of synthesized heterocyclic compounds with amino acids present in the active site of target enzyme (lanosterol 14 alpha demethylase). Absorption, distribution, metabolism, and excretion (ADME) analysis was indicative of drug-likeliness of the synthesized compounds.
The double composite layer composed of europium and terbium doped zinc oxide (Eu3+,Tb3+@ZnO) as downconversion material (DC) and neodymium and ytterbium-doped zinc oxide (Nd3+,Yb3+@ZnO) as upconversion materials (UC) was prepared and used as photoanodes to achieve the higher photovoltaic efficiency of dye sensitized solar cell(DSSCs). The double composite layer FTO/Eu3 + ,Tb3+@ZnO/TiO2/ Nd3+,Yb3+@ZnO have two disparate units; one provide downconversion luminescence by Ultraviolet excitation assigned to 7F0-5L6 of Eu3+, 7D4-7F5, of Tb3+, 5D4-7F4 of Tb3+, 7F0-5D1 of Eu3+ and other gives upconversion luminescence (λex = 980 nm) attributed to 4F7/2-4I15/2, 2H11/2-4I15/2, 4S3/2-4I15/2, 4F9/2-4I15/2. The photoelectric efficiency of double composite layer device E (FTO/Eu3+,Tb3+@ZnO/TiO2/Nd3+,Yb3+@ZnO) attains 2.68%, notably higher than device with undoped zinc oxide (ZnO). Higher efficiency in device E was due to enhancement of the light harvesting achieved by down converters and upconverters by converting Ultraviolet (UV) and near infrared (NIR) radiations to visible emission respectively. Furthermore, Eu3+,Tb3+@ZnO acts as confinement layer which suppresses the dark current and also inhibits the charge recombination.
Nd3+/Yb3+ co-doped NaGdF4@CaF2:Eu3+ nanoparticles were prepared through oleic acid/1-octadecene based coprecipitation method. Their structural characterizations were carried out by using powdered XRD pattern, SEM and TEM studies. The synthesized nanoparticles showed dual-mode emission i.e., visible and NIR emission and thus displayed a broad range of photoluminescence emission covering a visible red emission (618 nm) to near infrared first/second window emission (900, 990, 1062 and 1340 nm). Photoluminescence spectral studies showed highest emission intensity for NaGdF4:0.1Nd(3+),0.03Yb(3+)@CaF2:Eu3+. The color coordinates (x, y) for the visible emission of synthesized nanoparticles were calculated and the proposed energy transfer mechanism for NaGdF4:0.1Nd(3+),xYb(3+)@CaF2:Eu3+ nanoparticles was explained.
A series of Sm3+ and/or Eu3+ doped luminescent BaGdF5 nanophosphors were synthesized hydmthermally at 180 degrees C for 24 h using EDTA as chelating ligand. The structure of synthesized nanophosphors was confirmed by XRD pattern, SEM and TEM studies. The Sm3+ and/or Eu3+ doped BaGdF5 nanophosphors showed irregular sphere like morphology. The minimum average particle size was about 105 nm. The multicolor luminescence was obtained upon excitation at 272 nm depending on the dopant lanthanide ions. The luminescence decay profile of BaGdF5:Sm3+,Eu3+ nanophosphors with different concentrations of Eu3+ ions were obtained by monitoring emission due to magnetic dipole transition at 589 nm for Sm3+ ions. The highest luminescence intensity was obtained for BaGdF5:0.03Sm(3+),0.04Eu(3+) nanophosphor as a result of efficient energy transfer from Gd3+ to Sm3+ ions and Sm3+ to Eu3+ ions. The color coordinates for all the synthesized nanophosphors were calculated and represented in the form of CIE chromaticity diagram. The energy transfer mechanism for nanophosphors was also explained.
Oxidative amidation reaction of aldehydes with amines, bytertbutyl hydrogen peroxide in toluene was achieved. The reaction utilised thein situgenerated catalyst produced by Fe(II) - hydride complex [FeH2(PPh3)(4)], and N-heterocyclic carbene (NHC) ligand. The catalytic system was found efficient for the synthesis of wide variety of mono and disubstiuted amides.
Epoxy resins have been widely used for coatings, adhesives, electronic materials, and matrices for fiber-reinforced composites because of their outstanding mechanical properties, good heat resistance, high adhesion strength, and high electrical resistance. The properties of cured epoxy resins are affected by the structure of epoxy resin, curing agents, additives, and curing process. An overview of the recent literature on new developments in epoxy monomers, curing agents, and fire-retardant additives is described. The literature sources are mostly taken from publications from 2006 and later. This entry discusses the latest advancements of phosphorus-containing fire retardants for electrical and electronic applications and compares them with commercially available ones. Silicon, boron, metals, or nitrogen-containing products and inorganic additives remain of great interest as supplementary materials to phosphorus fire retardants. The mechanism of thermal degradation and fire retardancy of phosphorus fire retardants in epoxy resins is also discussed.
Malaria is a life threatening disease caused by microscopic parasites called Plasmodium that are transmitted to human beings by mosquitoes. Single celled Eukaryotic plasmodium parasite is responsible to cause malaria in human beings and is transmitted by bite of Anopheles species mosquitoes. Resurgence of malaria towards the end of 20th Century is due to failure of its eradication completely. Parasite recurrence occurs due to high densities of parasite, low immunity and non opimized drug concentration. The ineffective eradications strategies were due to indefinable complex life cycle of Plasmodium and emergence of drugs resistant strains of Plasmodium falciparum (Pf) including Artemisinin and Artemisinin based combination therapy (ACT). The vector of the disease i.e. mosquitoes became resistive towards Pyrethroids, which are only class of insecticides recommended for vector control.
The ternary photocatalyst PEDOT@ZnO@MWCNTs was fabricated using chemical oxidative method of polymerization. The fabrication of the catalyst was further investigated using spectroscopic techniques namely UV-Visible, FT-IR, XRD and the surface morphology was explored by SEM and TEM. The photodegradation kinetics of the azo dye MO followed pseudo first order kinetics at different pH. The photodegradation of the dye was studied in presence of PEDOT@ZnO@MWCNTs on irradiation with visible source of light. The redox activity of the photocatalyst was investigated by cyclic voltammetric technique and the mechanism of the photocatalysis was established via electronic impedance study. The evaluated value of rate constant, half life time period and the degradation efficiency sustenance the competence of the photocatalyst for the photodegradation of MO at the optimum pH value of 3.5. The chemical oxygen demand (COD) analysis was also favored the mineralization of the dye in presence of photocatalyst.