Search Results (717)

A series of 7-aminopyrazolo[1,5-d][1,2,4]triazin-4(5H)-ones was synthesized via a cascade condensation of methyl aroylpyruvates with 1,3-diaminoguanidine hydrochloride. The scope and limitations of this approach were investigated. Methyl mesitoylpyruvate bearing a sterically hindered mesityl substituent diverted the reaction pathway, affording a 1,2,4-triazine derivative. Diethyl 2,4,6-trioxoheptanedioate resulted in an unexpected pyrazolo[1,5-d][1,2,4]triazepine scaffold. All synthesized compounds were evaluated for growth-regulating activity using the green microalga Chlorella vulgaris as a model organism. 7-Amino-2-(4-methoxyphenyl)pyrazolo[1,5-d][1,2,4]triazin-4(5H)-one has shown the best results in the initial microplate screening, showing increased cell density at 10 μmol/L. However, subsequent validation in 50 mL flask cultures revealed no significant effect on biomass accumulation, photosynthetic pigment content, carbohydrate levels, or neutral lipid production compared to the negative control. Only a modest increase in protein content was observed at the concentration of 100 μmol/L. Full article

Type 2 diabetes (T2D), a major global health challenge, represents approximately 96% of all cases of diabetes worldwide. Epidemiological forecasts indicate the prevalence of this disease could rise by almost 45% over the next 25 years. T2D is a chronic metabolic disorder characterised by insulin resistance and progressive impairment of β-cell function. Untreated T2D can lead to serious microvascular and macrovascular complications. Traditional therapies have focused primarily on glycaemic control, whereas modern treatment strategies are increasingly centred on the broader pathophysiology of T2D. Among new therapeutic approaches, triazine derivatives have gained significant attention as versatile scaffolds for the development of antidiabetic drugs. This article provides a comprehensive review of triazines (mainly 1,2,4-triazines and 1,3,5-triazines) as promising compounds for the treatment of T2D and its complications. Three databases (Scopus, PubMed, and Web of Science) were searched for the period of 2000–2025. Over the past 25 years, numerous compounds have been described. They were primarily investigated as inhibitors of digestive enzymes and factors that cause diabetic complications. The individual sections discuss the biological activity of these compounds, focusing on SAR analysis and the studies conducted (in vitro, in silico, and in vivo). During this period, two compounds, fotagliptin and imeglimin, have entered clinical use. The results show that triazines have great potential to become antidiabetic drugs. They can not only regulate blood sugar levels (by acting on digestive enzymes, insulin secretion or glucose transport) but also directly prevent serious complications of diabetes. Full article

Background/Objectives: Lavandula cariensis species is cultivated uncommonly in the western region of Turkey. The colloquial appellations avayianos, karabasi, and myra are used to refer to the L. cariensis plant. The essential oil of L. cariensis was studied for its potential antiglaucoma, antioxidant, antidiabetic, and acetylcholinesterase inhibitory effects. Methods: The inhibitory effect of the essential oil of L. cariensis on the acetylcholinesterase (AChE), carbonic anhydrase II (CA II), and α-amylase enzymes was determined. Therefore, chemical profiles of L. cariensis’ essential oil were identified using Gas Chromatography Mass Spectrometry (GC-MS) and as Chromatography with Flame Ionization Detection (GC-FID) analyses. Results: Camphor (39.73%), fenchone (19.49%), exobornyl acetate (6.81%), camphene (5.49%), and eucalyptol (5.49%) were the most abundant compounds in L. cariensis essential oil. Radical scavenging effect of the essential oil of L. cariensis was examined using 1,1-diphenyl-2-picrylhydrazyl (DPPH) (IC₅₀: 231.0 ± 0.094 μg/mL) and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) (IC₅₀: 7.45 ± 0.013 μg/mL) radicals. Also, the ferric ions (Fe³⁺), cupric ions (Cu²⁺), and Fe³⁺-2,4,6-tri(2-pyridyl)-S-triazine (TPTZ) complex reducing capabilities were studied. Additionally, essential oil of L. cariensis indicated a comparable level of inhibition towards hCA II (IC₅₀: 276.42 μg/mL), AChE (IC₅₀: 14.22 μg/mL), and α-amylase (IC₅₀: 475.63 μg/mL) enzymes. Conclusions: The evaluation of the antioxidant capabilities and enzyme inhibition profiling of the essential oil of L. cariensis will be made possible by this comprehensive study, which serves as a springboard for further research. The essential oil of L. cariensis demonstrated enzyme-inhibitory activities against target enzymes associated with Alzheimer’s disease, diabetes, and glaucoma. Also, this study’s in vitro inhibition suggests promising prospects. Full article

In searching for novel molecules to act as antibacterial agents, particularly against Mycobacterium tuberculosis bacteria, three series of C5- and C6-substituted 1,2,3-triazine compounds were investigated: 1,2,3-triazine-4-carboxylate 1-oxide (series 1), 1,2,3-triazine-4-carboxylate (series 2), and 3,6-dihydro-1,2,3-triazine-4-carboxylate 1-oxide derivatives (series 3). Their structural elucidation was confirmed by ¹H-NMR, ¹³C-NMR, and HRMS. We determined their antibacterial activity (MIC value) using the MABA against the M. tuberculosis H37Rv strain, as well as their physicochemical and pharmacokinetic properties. Finally, to determine their potential mode of action, an inhibition assay against M. tuberculosis DNA gyrase was performed. Compounds 4-ethoxycarbonyl-5-(3-methoxyphenyl)-1,2,3-triazine (2l) and 4-ethoxycarbonyl-5 -(n-propyl)-1,2,3-triazine (3s) exhibited high activity against M. tuberculosis with MIC values < 5.90 µg/mL and selectivity index of 18.56 and 8.36, respectively. Additionally, compound 2m also exhibited anti-mycobacterial activity with MIC values < 10.0 µg/mL. However, none of the selected compounds inhibited the activity of M. tuberculosis DNA gyrase, suggesting that another drug target may be involved as a mode of action. These results encourage exploring the use of 1,2,3-triazine as a scaffold for the development of new anti-mycobacterium agents. Full article

Heavy metal contamination in water remains a major environmental concern due to the persistence, toxicity, and bioaccumulation potential of metal ions such as Ni²⁺ and Cu²⁺. Therefore, the development of sustainable membrane materials with improved permeability and metal ion retention capacity is of significant interest for advanced water purification applications. In this research, crown ether-functionalized cellulose acetate membranes were developed by employing cyanuric chloride as a linker in order to enable advanced heavy metal ion retention capacity. In order to achieve this, the modification process involved a multi-step approach comprising successive hydroxylation, silanization, triazine activation, and crown ether grafting. The successful functionalization was confirmed by FTIR (Fourier Transform Infrared Spectroscopy) and XPS (X-ray Photoelectron Spectroscopy) analyses, while thermal characterization demonstrated improved stability over a wide range of temperatures without compromising the integrity of the cellulose acetate backbone. The crown-ether-functionalized membranes exhibited enhanced performance in terms of heavy metal ion separation, demonstrating significantly higher retention of Ni²⁺ (30%) and Cu²⁺ (27%) as compared to pristine CA membranes (<10%) over repeated filtration cycles. These results demonstrate that crown ether functionalization is a versatile approach for tuning the interfacial features of cellulose acetate membranes in order to achieve increased permeability and selectivity toward heavy metal removal, highlighting their potential for advanced water purification applications. Full article

A hybrid method combining biomimetic liquid chromatography with immobilized artificial membrane (IAM) and quantitative structure–activity relationships (QSARs) was used to derive helpful models for predicting selected properties related to distribution (binding to human serum albumin (log P_w/HSA)) and absorption (skin permeation (log K_w/sp), plant cuticle permeation (log P_w/pc), and human intestinal permeability (Caco-2)), and therefore influencing the effectiveness or unwanted effects of 199 synthetic compounds that are regarded as potential drugs or plant protection products. The molecules under investigation—derivatives of 5H-6,7-dihydroimidazo [2,1-c][1,2,4]triazole, 7,8-dihydroimidazo[2,1-c][1,2,4]triazin-4(6H)-one, 2,6,7,8-tetrahydroimidazo[2,1-c][1,2,4]triazine-3,4-dione, 1H-1,2,4-triazole, carbamic and phenoxyacetic acid—differ in their properties but all meet the requirements for xenobiotics to be considered as medicinal products. Reliable high-concept models were developed, indicating lipophilicity, molecular size, electronic properties, and the number of rotatable bonds as descriptors that determine the biological properties of these compounds. These models have been optimized and cross-validated, confirming their reliability and high predictivity. Full article

Emissions of carbon dioxide are considered to be the major factors leading to climate change. Current technologies for CO₂ capture include chemical and physical absorption, membrane separation, and cryogenic distillation. Solid adsorbents are highly effective, and emerging porous liquids—solid adsorbents dispersed in a compatible liquid—represent a promising alternative for CO₂ capture. In this study, commercial and synthetic porous carbon nanomaterials were dispersed in a 1 wt.% aqueous solution of sodium dodecyl sulfate and compared on the efficiency of CO₂ uptake. The experimental results confirmed that CO₂ uptake is enhanced in porous liquids employing surface-modified carbon nanotubes (69 mmol/L) and covalent triazine frameworks, with triazine-based nanomaterials exhibiting superior CO₂ uptake performance (76 and 82 mmol/L) due to their increased polar group number. Full article

Simazine (SIM), a triazine herbicide and potential environmental risk factor, has been associated with neurotoxicity; however, the underlying mechanisms remain poorly characterized. Salidroside (SAL), a natural antioxidant with mitochondrial protective properties, has been reported to alleviate SIM-induced neuronal injury. Using an integrated strategy combining network toxicology and network pharmacology with experimental validation, this study systematically investigated the neurotoxic mechanisms of SIM and the neuroprotective effects of SAL. Bioinformatics analyses revealed that SIM- and SAL-related targets were significantly enriched in apoptosis- and autophagy-associated pathways. In vitro experiments demonstrated that SIM induced mitochondrial structural damage, metabolic dysfunction, and dopaminergic neuron-like SH-SY5Y cells apoptosis by inhibiting PINK1/Parkin-mediated mitophagy. Conversely, SAL effectively protected SH-SY5Y cells against SIM-induced neurotoxicity by restoring PINK1/Parkin signaling, thereby enhancing mitophagy and suppressing apoptosis. The present study elucidates the central mechanism of SIM-induced PD-like neurotoxicity in vitro and, for the first time, confirms the potential protective effect of SAL. These findings provide a novel theoretical basis for investigating nerve injury induced by SIM exposure and underscore the potential of plant-derived compounds in preventing nerve injuries related to environmental toxicants. Full article

This study presents the synthesis of novel heterocyclic derivatives from oxazol-5(4H)-ones and 1,2,4-triazin-6(5H)-ones classes containing the 4-chlorophenylsulfonylphenyl and arylidene motifs as potential bioactive molecules. The synthesis of new oxazol-5(4H)-ones was conducted by cyclocondensation of 2-(4-(4-chlorophenylsulfonyl)benzamido)acetic acid with several aromatic aldehydes. The reaction of oxazol-5(4H)-ones with phenylhydrazine afforded the new 1,2,4-triazin-6(5H)-ones. Spectroscopic techniques (IR, ¹H-, ¹³C-NMR, and MS) and elemental analysis were used to confirm the structures of all new compounds. The compounds were tested against Saccharomyces cerevisiae, and cells lacking the BLH1 gene were more susceptible to compound toxicity. Moreover, the compounds increased bleomycin toxicity against yeast cells. Structural similarity analysis against the ChEMBL database and approved drugs from DrugBank was performed to evaluate the structural novelty of the synthesized compounds and to obtain preliminary information regarding their potential pharmacological profiles. Full article

Eminium rauwolffii (Blume) Schott var. rauwolffii is a member of the Araceae a large and mainly tropical family distributed worldwide. The Eminium species are utilized for various purposes including therapeutic uses in traditional medicine and as food. To analyze the antioxidant properties of water extract of E. rauwolffii (WEER) and ethanol extract of E. rauwolffii (EEER), 2,2’-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS^•+) radical and 1,1-diphenyl-2-picrylhydrazyl (DPPH^.) free radical scavenging, Fe³⁺-2,4,6-tris(2-pyridyl)-S-triazine (TPTZ) and Cu²⁺ reducing assays were studied. Antioxidant activities and reducing properties of both extracts were compared to standard antioxidants: BHT, BHA, α-Tocopherol, and Trolox. The IC₅₀ values of EEER for radical scavenging were higher than those of standard antioxidants (25.35 ± 1.42 μg/mL for ABTS^•+ and 106.80 ± 1.88 μg/mL for DPPH^•). The total phenolic and flavonoid quantities in WEER and EEER were measured in the range of 189.78 ± 0.01 to 298.54 ± 0.01 mg GAE/g and 89.37 ± 0.01 to 178.95 ± 0.01 mg QE/g, respectively. The IC₅₀ values for EEER and WEER against α-glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and carbonic anhydrase I and II (hCA I and II) enzymes were 10.79 ± 5.61 to 13.18 ± 5.77, 36.14 ± 4.61 to 62.63 ± 1.67, 69.37 ± 7.36 to 37.48 ± 0.27, 81.30 ± 5.95 to 62.35 ± 8.03, and 29.34 ± 1.38 to 115.90 ± 3.3 µg/mL respectively. The antioxidant activity and enzymes inhibitory capacity of WEER were close, and comparable to the capacity demonstrated by the standards. The amount of sixteen compounds was identified from EEER. Numerous phytochemicals, including cynaroside, p-coumaric acid, cosmosiin, caffeic acid, and quinic acid, were quantitatively determined using the LC-MS/MS method. This clearly indicates that phenolic- and flavonoid-rich E. rauwolffii may have potential in the management of glaucoma, Alzheimer’s disease, diabetes, cardiovascular, and cancer disorders. Full article

Ultraviolet (UV) radiation is a recognized human carcinogen, and topical sunscreens remain the primary strategy for photoprotection. As community pharmacies represent trusted sources of skincare products, evaluating the composition of sunscreens distributed through this channel is particularly relevant. This cross-sectional market analysis investigated UV filters used in sunscreen products available in Lithuanian community pharmacies in November–December 2025. Products were identified through online pharmacy catalogs and assessed for labeled Sun Protection Factor (SPF), number and type of UV filters, and filter combinations in accordance with Regulation (EC) No 1223/2009. A total of 467 products from 98 brands were included, and 26 distinct UV filters were identified. Triazine derivatives predominated, particularly bis-ethylhexyloxyphenol methoxyphenyl triazine (64.67%) and ethylhexyl triazone (58.03%). Most products (61.67%) were labeled SPF ≥ 50 and contained multiple UV filters (mean 4.29 ± 1.66), with significantly more filters in SPF ≥ 50 formulations (p < 0.001). These results indicate that sunscreen products available in Lithuanian pharmacies are dominated by high-SPF formulations and selective multi-filter systems, providing region-specific insights relevant to regulatory oversight and consumer exposure assessment. Full article

In recent decades, triazine herbicides (THs), one of the most widely used agrochemicals, have been extensively applied to enhance crop yields. However, their persistent nature and high mobility have resulted in pervasive contamination of aquatic ecosystems, posing significant risks to non-target organisms and human health through bioaccumulation and endocrine disruption. Addressing THs pollution in water bodies has thus emerged as a critical environmental challenge. This study reviews the efficacy of biochar, a carbon-rich material derived from biomass pyrolysis, for TH removal due to its high surface area, hierarchical porosity, and tunable surface functionality. The maximum reported adsorption capacities are up to 260.5 mg·g⁻¹; with degradation efficiencies, they can exceed 99.5% in advanced oxidation systems. Mechanistic investigations reveal that TH removal primarily involves π–π interactions, hydrogen bonding, pore filling, and electrostatic attraction during adsorption, while degradation proceeds via radical pathways (e.g., •OH, SO₄^•−) and nonradical routes (e.g., ¹O₂, direct electron transfer) in processes such as persulfate activation, photocatalysis, and Fenton-like reactions. By analyzing degradation intermediates and pathways, this review underscores the necessity of coupling adsorption with advanced oxidation to achieve complete mineralization and mitigate secondary ecological risks. Furthermore, it emphasizes the importance of tailoring biochar’s physicochemical properties through feedstock selection, pyrolysis conditions, and chemical modifications to optimize THs’ removal performance. This work advocates for the integration of biochar-based technologies into sustainable water treatment frameworks, aligning with carbon neutrality goals and circular economy principles. Future research should prioritize scalable synthesis methods, long-term stability assessments, and field-scale validations to translate laboratory insights into practical solutions for safeguarding global water resources. However, realizing this potential requires that we overcome challenges related to matrix interference, catalyst deactivation, and incomplete mineralization, which are often overlooked in laboratory-scale studies. Full article

Ixora chinensis Lam. has traditionally been used to treat conditions such as acne, high blood pressure, bleeding, tuberculosis, and rheumatism. This study aimed to investigate the methanolic extract of I. chinensis leaves to determine their bioactive compounds and evaluate their effects on both central and peripheral pain using in vivo and in silico approaches. The GC-MS analysis revealed 41 phytochemicals, including 14 phenolics, 4 esters, 12 terpenoids, 8 alkaloids, and 3 sulfur-containing compounds. In the glucose tolerance test, both the chloroform-soluble fraction (CF) and n-hexane fraction (NHF) exhibited p < 0.05 reductions in blood glucose levels at a dosage of 400 mg/kg with decreases of 51.94% and 46.63%, respectively, compared to the positive control (64.02%). The central analgesic evaluation showed significant (p < 0.001) enhancements in tail-flick latency for the fraction (184.94%) and CF (170.51%) following 90 min. In the pain relief assay, NHF showed inhibition (64.33%, p < 0.001) followed by an aqueous fraction (57.35%). These pharmacological findings were supported by in silico analysis. Concerning activity, 5-(dimethylamino)-1- acid phenyl ester (−8.9 kcal/mol) and 9,9-dimethyl-9H-fluoren-3-ol (−8.4 kcal/mol) displayed the strongest binding affinity to AMPK. Additionally, 2,3-diphenyl-2-cyclopropen-1-one exhibited favorable interactions with α-amylase (−8.0 kcal/mol) and α-glucosidase (−8.3 kcal/mol). Similarly, the central analgesic effect correlated with the strong μ-opioid receptor affinity of s-Triazine, 2-amino-4-(piperidinomethyl)-4-piperidino (−8.8 kcal/mol). N-Methyl-N-(4-toluenesulfonyl)-benzamide (−8.6 kcal/mol) and s-Triazine derivative (−8.9 kcal/mol) demonstrated notable COX-1 and COX-2 inhibition potential. Overall, the findings indicate I. chinensis leaves as a promising source of bioactive compounds with significant antihyperglycemic and analgesic properties. Full article

Triazine herbicides are widely used for weed control in agricultural systems, and their occurrence in water bodies has been frequently reported worldwide. This study assessed the efficiency of a hydrochar derived from the epicarp and mesocarp of passion fruit residues for the removal of three triazine herbicides (atrazine, ametryn, and metribuzin), with the aim of developing a material suitable for application in water remediation programs. The adsorption capacity of biomass and hydrochar derived from passion fruit residues was evaluated with and without activation using 0.5 mol L⁻¹ phosphoric acid. The adsorption of herbicides was not significantly affected by pH within the range of 4 to 8. The acid hydrochar, which exhibited the highest removal capacity among the evaluated adsorbents, presented adsorption capacities of 18.05, 10.83, and 5.05 µg g⁻¹ for atrazine, ametryn, and metribuzin, respectively. These values correspond to removal efficiencies of approximately 62%, 72%, and 52% at initial concentrations of 0.33, 0.25, and 0.15 mg L⁻¹. The adsorption equilibrium time varied among the herbicides, reaching 4 h for atrazine and ametryn and 5 h for metribuzin. The adsorption dynamics between the adsorbents and adsorbates were best described by the pseudo-second-order kinetic model for ametryn and metribuzin, while atrazine had a higher correlation with the Elovich equation. The Weber–Morris model did not adequately describe the adsorption process. Among the isotherms tested, the Freundlich model provided the best fit for all three herbicides. The desorption rates of the acid hydrochar were 51%, 13%, and 83% for atrazine, ametryn, and metribuzin, respectively. Therefore, hydrochar derived from passion fruit residues represents a promising alternative for the remediation of triazine herbicides. Full article