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1.
Heliyon ; 10(3): e25521, 2024 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-38356588

RESUMO

Nanomaterials (NMs) have garnered significant attention in recent decades due to their versatile applications in a wide range of fields. Thanks to their tiny size, enhanced surface modifications, impressive volume-to-surface area ratio, magnetic properties, and customized optical dispersion. NMs experienced an incredible upsurge in biomedical applications including diagnostics, therapeutics, and drug delivery. This minireview will focus on notable examples of NMs that tackle important issues, demonstrating various aspects such as their design, synthesis, morphology, classification, and use in cutting-edge applications. Furthermore, we have classified and outlined the distinctive characteristics of the advanced NMs as nanoscale particles and hybrid NMs. Meanwhile, we emphasize the incredible potential of metal-organic frameworks (MOFs), a highly versatile group of NMs. These MOFs have gained recognition as promising candidates for a wide range of bio-applications, including bioimaging, biosensing, antiviral therapy, anticancer therapy, nanomedicines, theranostics, immunotherapy, photodynamic therapy, photothermal therapy, gene therapy, and drug delivery. Although advanced NMs have shown great potential in the biomedical field, their use in clinical applications is still limited by issues such as stability, cytotoxicity, biocompatibility, and health concerns. This review article provides a thorough analysis offering valuable insights for researchers investigating to explore new design, development, and expansion opportunities. Remarkably, we ponder the prospects of NMs and nanocomposites in conjunction with current technology.

2.
Med Chem ; 15(2): 175-185, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30207240

RESUMO

BACKGROUND: Barbituric acid derivatives are a versatile group of compounds which are identified as potential pharmacophores for the treatment of anxiety, epilepsy and other psychiatric disorders. They are also used as anesthetics and have sound effects on the motor and sensory functions. Barbiturates are malonylurea derivatives with a variety of substituents at C-5 position showing resemblance with nitrogen and sulfur containing compounds like thiouracil which exhibited potent anticancer and antiviral activities. Recently, barbituric acid derivatives have also received great interest for applications in nanoscience. OBJECTIVE: Synthesis of 5-arylidene-N,N-diethylthiobarbiturates, biological evaluation as potential α-glucosidase inhibitors and molecular modeling. METHODS: In the present study, N,N-Diethylthiobarbituric acid derivatives were synthesized by refluxing of N,N-diethylthiobarbituric acid and different aromatic aldehydes in distilled water. In a typical reaction; a mixture of N,N-diethylthiobarbituric acid 0.20 g (1 mmol) and 5-bromo-2- hydroxybenzaldehyde 0.199 g (1 mmol) mixed in 10 mL distilled water and reflux for 30 minutes. After completion of the reaction, the corresponding product 1 was filtered and dried and yield calculated. It was crystallized from ethanol. The structures of synthesized compounds 1-25 were carried out by using 1H, 13C NMR, EI spectroscopy and CHN analysis used for the determination of their structures. The α-glucosidase inhibition assay was performed as given by Chapdelaine et al., with slight modifications and optimization. RESULTS: Our newly synthesized compounds showed a varying degree of α-glucosidase inhibition and at least four of them were found as potent inhibitors. Compounds 6, 5, 17, 11 exhibited IC50 values (Mean±SEM) of 0.0006 ± 0.0002, 18.91 ± 0.005, 19.18 ± 0.002, 36.91 ± 0.003 µM, respectively, as compared to standard acarbose (IC50, 38.25 ± 0.12 µM). CONCLUSION: Our present study has shown that compounds 6, 5, 17, 11 exhibited IC50 values of 0.0006 ± 0.0002, 18.91 ± 0.005, 19.18 ± 0.002, 36.91 ± 0.003 µM, respectively. The studies were supported by in silico data analysis.


Assuntos
Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/farmacologia , Simulação de Acoplamento Molecular , Tiobarbitúricos/síntese química , Tiobarbitúricos/farmacologia , alfa-Glucosidases/metabolismo , Técnicas de Química Sintética , Desenho de Fármacos , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/metabolismo , Conformação Proteica , Relação Estrutura-Atividade , Tiobarbitúricos/química , Tiobarbitúricos/metabolismo , alfa-Glucosidases/química
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