Recent updates on 1,2,3-triazole-containing hybrids with in vivo therapeutic potential against cancers: A mini-review

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 251, С. 115254 - 115254

Опубликована: Март 6, 2023

Язык: Английский

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Recent Trends in the Synthesis and Bioactivity of Coumarin, Coumarin–Chalcone, and Coumarin–Triazole Molecular Hybrids

Molecules, Год журнала: 2024, Номер 29(5), С. 1026 - 1026

Опубликована: Фев. 27, 2024

Molecular hybridization represents a new approach in drug discovery which specific chromophores are strategically combined to create novel drugs with enhanced therapeutic effects. This innovative strategy leverages the strengths of individual address complex biological challenges, synergize beneficial properties, optimize pharmacokinetics, and overcome limitations associated single-agent therapies. Coumarins documented possess several bioactivities have therefore been targeted for combination other active moieties molecular hybrids. review summarizes recent (2013–2023) trends synthesis coumarins, as well coumarin–chalcone coumarin–triazole To cover wide aspects this area, we included differently substituted chalcones, 1,2,3– 1,2,4–triazoles considered point fusion/attachment coumarin show diversity these The reported syntheses mainly relied on well-established chemistry without need strict reaction conditions usually produced high yields. Additionally, discussed compounds, including antioxidative, antimicrobial, anticancer, antidiabetic, anti-cholinesterase activities commented their IC50 where possible. Promising bioactivity results obtained so far. It is noted that mechanistic studies infrequently found published work, was also mentioned give reader better understanding. aims provide valuable information enable further developments field.

Язык: Английский

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Synthesis of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazine-1,2,3-triazoles as potent EGFR targeting anti-breast cancer agents

Journal of Molecular Structure, Год журнала: 2024, Номер 1306, С. 137803 - 137803

Опубликована: Фев. 14, 2024

Язык: Английский

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A Review of Click Chemistry in the Synthesis of Organophosphorus Triazoles and Their Biological Activities

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер 286, С. 117270 - 117270

Опубликована: Янв. 13, 2025

Organophosphorus compounds, characterized by the incorporation of phosphorus into organic molecules, play a critical role in various fields such as medicine, agriculture, and industry. Their unique electronic properties versatility make them essential developing therapeutic agents, pesticides, materials. One prominent class organophosphorus compounds is heterocycles, which combine benefits both cyclic structures. Triazoles, nitrogen-containing heterocyclic are particularly notable for their broad biological activities, including anticancer, antiviral, antibacterial, antioxidant effects. Traditional methods synthesizing triazoles often encounter challenges low yields non-selective products, whereas click chemistry provides more efficient reliable alternative. The copper-catalyzed azide-alkyne [3 + 2] cycloaddition, cornerstone chemistry, allows rapid selective formation under mild conditions. When functionalized with groups, not only retain but enhance improving potency, selectivity, stability. This review covers synthesis organophosphorus-functionalized via explores molecular structure, coordination these compounds. behavior interactions derivatives metal ions also addressed, significantly influence chemical reactivity, stability, bioactivity.

Язык: Английский

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Antibacterial and antibiofilm activity of permanently ionized quaternary ammonium fluoroquinolones

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 254, С. 115373 - 115373

Опубликована: Апрель 14, 2023

A series of quaternary ammonium fluoroquinolones was obtained by exhaustive methylation the amine groups present at 7-position fluoroquinolones, including ciprofloxacin, enoxacin, gatifloxacin, lomefloxacin, and norfloxacin. The synthesized molecules were tested for their antibacterial antibiofilm activities against Gram-positive Gram-negative human pathogens, i.e. Staphylococcus aureus Pseudomonas aeruginosa. study showed that compounds are potent agents (MIC values lowest 6.25 μM) with low cytotoxicity in vitro as assessed on BALB 3T3 mouse embryo cell line. Further experiments proved derivatives able to bind DNA gyrase topoisomerase IV active sites a fluoroquinolone-characteristic manner. most contrast reduce total biomass P. aeruginosa ATCC 15442 biofilm post-exposure experiments. latter effect may be due dual mechanism action which also involves disruption bacterial membranes. IAM-HPLC chromatographic immobilized artificial membranes (phospholipids) those moderate lipophilicity containing cyclopropyl group N1 nitrogen atom fluoroquinolone core.

Язык: Английский

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1,2,3-Triazoles and their metal chelates with antimicrobial activity

Frontiers in Chemistry, Год журнала: 2023, Номер 11

Опубликована: Авг. 10, 2023

The emergence of drug-resistant bacterial and fungal pathogens has highlighted the urgent need innovative antimicrobial therapeutics. Transition metal complexes with biologically active ligands (coumarins, terpyridines, triazoles, uracils, etc.) have long been investigated for activity. 1,2,3-Triazoles their molecular derivatives are well known a plethora physiological activities, including antibacterial antifungal. aim present mini-review is to inform reader about research conducted on potential 1,2,3-triazole transition metals. What authors find surprising how little such experimentation actually performed reported in scientific literature. goal highlight efforts up now impress upon vast perspectives novel, effective medicinal substances hidden this yet unexplored field.

Язык: Английский

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Synthesis of 1,2,3-triazole-piperazin-benzo[b][1,4]thiazine 1,1-dioxides: antibacterial, hemolytic and in silico TLR4 protein inhibitory activities

RSC Advances, Год журнала: 2024, Номер 14(13), С. 8921 - 8931

Опубликована: Янв. 1, 2024

Novel 1,2,3-triazoles (6a–6j & 8a–8g) were synthesized and evaluated for their antibacterial activity against S. aureus . The more potent compounds further in silico TLR4 inhibitory activity.

Язык: Английский

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Molecular hybrid of 1,2,3-triazole and schiff base as potential antibacterial agents: DFT, molecular docking and ADME studies

Journal of Molecular Structure, Год журнала: 2023, Номер 1286, С. 135617 - 135617

Опубликована: Апрель 20, 2023

Язык: Английский

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Anti-cancer activity of synthetic gefitinib-1,2,3-triazole derivatives against Hela cells via induction of apoptosis

Frontiers in Chemistry, Год журнала: 2025, Номер 13

Опубликована: Янв. 24, 2025

Cervical cancer ranks as the fourth most common among women. However, current treatments have significant side effects and limited therapeutic on advanced diseases, so it is necessary to discover better for cervical cancer. The study investigated potential anticancer of a series gefitinib-1,2,3-triazole derivative Hela cells. Among investigated, target compound c13 showed good activity against cells (IC 50 = 5.66 ± 0.35 μM) compared with gefitinib 14.18 3.19 μM). Moreover, significantly inhibited colony formation ability in dose-dependent manner, accompanied by morphological changes HeLa Further investigations demonstrated that triggered cell apoptosis arrested cycle at G2/M phase In addition, western blot analysis revealed upregulated Bax/Bcl-2 ratio, increased levels active caspase 3 PARP1 cleavage, which suggested involvement mitochondrial pathway -induced apoptosis. brief, these results indicated promising treatment

Язык: Английский

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Design, one-pot synthesis, in silico ADMET prediction and molecular docking of novel triazolyl thiadiazine and thiazole derivatives with evaluation of antimicrobial, antioxidant and antibiofilm inhibition activity

Journal of the Iranian Chemical Society, Год журнала: 2023, Номер 20(12), С. 2923 - 2947

Опубликована: Окт. 13, 2023

Язык: Английский

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