Assessment of the In Vitro Biological Activities of Schiff Base-Synthesized Copper Oxide Nanoparticles as an Anti-Diabetic, Anti-Alzheimer, and Anti-Cancer Agent

Pharmaceutics, Год журнала: 2025, Номер 17(2), С. 180 - 180

Опубликована: Фев. 1, 2025

Background/Objectives: Numerous diseases such as diabetes, Alzheimer’s disease, and cancer have spread in the whole world, especially Arab world. Also, various applications of Schiff-base functionalized nanoparticles copper oxide (CuO-NPs) therapeutic been discovered. Thus, current research highlights (i) synthesis produced with a Schiff base (SB) serving capping agent during their (ii) assessment vitro biological activities base-synthesized (SB-CuO-NPs) (SB). Methods: SB-CuO-NPs were characterized using ultraviolet-visible (UV-Vis) spectroscopy, zeta potential, DLS analysis, transmission electron microscope (TEM). It also focuses on assessing activities, including antioxidant, scavenging, anti-diabetic, anti-Alzheimer, anti-arthritic, anti-inflammatory, cytotoxic enzymes inhibitory methods described literature. Results: The results compared those SB. demonstrated superior when to SB from which they produced. Conclusions: this investigation concluded that CuO-NPs, synthesized an alternative agent, exhibited enhanced efficacy relative original In future, efficiency against Alzheimer’s, will be assessed experimental animals (in vivo).

Язык: Английский

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Explore new quinoxaline pharmacophore tethered sulfonamide fragments as in vitro α‐glucosidase, α‐amylase, and acetylcholinesterase inhibitors with ADMET and molecular modeling simulation

Drug Development Research, Год журнала: 2024, Номер 85(4)

Опубликована: Июнь 1, 2024

Abstract A new series of quinoxaline‐sulfonamide derivatives 3 – 12 were synthesized using fragment‐based drug design by reaction quinoxaline sulfonyl chloride (QSC) with different amines and hydrazines. The evaluated for antidiabetic anti‐Alzheimer's potential against α‐glucosidase, α‐amylase, acetylcholinesterase enzymes. These showed good to moderate potency α‐amylase α‐glucosidase inhibitory percentages between 24.34 ± 0.01%–63.09 0.02% 28.95 0.04%–75.36 0.01%, respectively. Surprisingly, bis ‐sulfonamide derivative 4 revealed the most potent activity 75.36 0.01% 63.09 α ‐glucosidase compared acarbose (IP = 57.79 67.33 0.01%), Moreover, exhibited as a minute decline from compound 44.93 38.95 0.01%. Additionally, in vitro designed weak activity. Still, sulfonamide‐quinoxaline emerged active member percentage 41.92 donepezil 67.27 0.60%). DFT calculations, docking simulation, target prediction, ADMET analysis performed discussed detail.

Язык: Английский

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Exploring the Potential Biological Activities of Pyrazole-Based Schiff Bases as Anti-Diabetic, Anti-Alzheimer’s, Anti-Inflammatory, and Cytotoxic Agents: In Vitro Studies with Computational Predictions

Pharmaceuticals, Год журнала: 2024, Номер 17(5), С. 655 - 655

Опубликована: Май 17, 2024

In this innovative research, we aim to reveal pyrazole-based Schiff bases as new multi-target agents. context, re-synthesized three sets of bases, 5a–f, 6a–f, and 7a–f, evaluate their biological applications. The data from in vitro assays (including antioxidant scavenging activities, anti-diabetes, anti-Alzheimer’s, anti-inflammatory properties) the 7a–f showed that six 5a, 5d, 5e, 5f, 7a, 7f possess highest properties among compounds evaluated. cytotoxicity against lung (A549) colon (Caco-2) human cancer types, well normal (WI-38) cell lines, was investigation demonstrated 7a are active cells, while two 5e exhibited towards cells. Additionally, enzymatic activities caspase-3 Bcl-2 were Furthermore, assessed silico absorption, distribution, metabolism, toxicity (ADMT) more potent bases. After modifying structures plan further extend studies future.

Язык: Английский

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Advances in synthesis, medicinal properties and biomedical applications of Pyridine Derivatives: A Comprehensive Review

European Journal of Medicinal Chemistry Reports, Год журнала: 2024, Номер 12, С. 100210 - 100210

Опубликована: Сен. 6, 2024

Язык: Английский

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Bioactive Fused Pyrazoles Inspired by the Adaptability of 5-Aminopyrazole Derivatives: Recent Review

Molecules, Год журнала: 2025, Номер 30(2), С. 366 - 366

Опубликована: Янв. 17, 2025

Heterocyclic compounds, especially those containing the pyrazole moiety, are highly significant in organic chemistry and possess remarkable diverse biological properties. The 5-aminopyrazole derivatives key starting materials for synthesis of numerous bioactive compounds such as pyrazolopyridine, pyrazolopyrimidine, pyrazoloquinazoline, pyrazolotriazine derivatives. Many inspired by a wide spectrum activities medicinal applications antioxidants, anticancer agents, enzyme inhibitors, antimicrobials, anti-tuberculosis activities. This review summarizes recently reported methods fused pyrazole-based based on within last 5 years (2020 to present). One important goals this is illustrate future strategies design, development, utilization products potent drugs.

Язык: Английский

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In Vitro Enzymatic and Computational Assessments of Pyrazole–Isatin and Pyrazole–Indole Conjugates as Anti-Diabetic, Anti-Arthritic, and Anti-Inflammatory Agents

Pharmaceutics, Год журнала: 2025, Номер 17(3), С. 293 - 293

Опубликована: Фев. 23, 2025

Background/Objectives: Recently, the prevalence of diseases such as diabetes, arthritis, and inflammatory diseases, along with their complications, has become a significant health problem. This is in addition to various biomedical applications pyrazole, isatin, indole derivatives. Accordingly, cooperation will continue between chemistry scientists, pharmaceutical human doctors produce hybrid compounds from pyrazole isatin or possessing biological activities anti-diabetic, anti-arthritic, anti-inflammatory agents. Methods: The two series pyrazole–isatin conjugates 12a–h pyrazole–indole 14a–d were prepared our previous works via direct reaction 5-amino-pyrazoles 10a–d N-alkyl 11a,b, 1H-indole-3-carbaldehyde (13), respectively, using previously reported procedure. potential agents assessed through estimated inhibition percentage (%) median inhibitory concentrations (IC50) methods described literature. Further, computational assessments toxic doses (the lethal dose, LD50), toxicity classes, drug-likeness model scores (DLMS), molecular lipophilicity (MLP) maps, polar surface area (PSA) topological (TPSA) values predicted available free websites. Results: vitro enzymatic assessment results showed that conjugate 14b possesses powerful against (i) α-amylase (% = 65.74 ± 0.23, IC50 4.21 0.03 µg/mL) α-glucosidase 55.49 2.76 0.01 µg/mL); (ii) protein denaturation enzyme 49.30 0.17) proteinase 46.55 an value 6.77 µg/mL; (iii) COX-1, COX-2, 5-LOX enzymes 5.44 0.03, 5.37 0.04, 7.52 which almost close indomethacin zileuton drugs. Also, lipophilic properties thus can cross cell membranes, effective for treatment; all possess TPSA more than 140 Å2 good intestinal absorption. Conclusions: synthesized works. these concluded studied results. In future, research team present vitro, vivo biological, hopefully obtain effectual anti-inflammatory.

Язык: Английский

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Synthesis, biological evaluation, molecular docking analyses, and ADMET study of azo derivatives containing 1-naphthol against MβL-producing s. Maltophilia

Results in Chemistry, Год журнала: 2024, Номер unknown, С. 101864 - 101864

Опубликована: Окт. 1, 2024

Язык: Английский

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Analysis of skeletal diversity of multi-target directed ligands (MTDLs) targeting Alzheimer’s disease

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер 286, С. 117277 - 117277

Опубликована: Янв. 18, 2025

Язык: Английский

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Adenocarpine, Marmesin, and Lycocernuine from Ficus benjamina as Promising Inhibitors of Aldose Reductase in Diabetes: A Bioinformatics-Guided Approach

Applied Biochemistry and Biotechnology, Год журнала: 2025, Номер unknown

Опубликована: Янв. 21, 2025

Язык: Английский

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Computational characterization of phytochemical inhibitors targeting cathepsin B for potential cancer therapy: A multi-parametric approach involving molecular docking, DFT and MD simulations study

Journal of Molecular Liquids, Год журнала: 2025, Номер unknown, С. 127423 - 127423

Опубликована: Март 1, 2025

Язык: Английский

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