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1.
Heliyon ; 10(18): e37847, 2024 Sep 30.
Artículo en Inglés | MEDLINE | ID: mdl-39315144

RESUMEN

Developing highly sensitive and selective non-enzymatic electrochemical biosensors for disease biomarker detection has become challenging in healthcare applications. However, advances in material science are opening new avenues for creating more dependable biosensing technologies. In this context, the present work introduces a novel approach by engineering a hybrid structure of zinc oxide nanorod (ZnO NR) modified with iron oxide nanoparticle (Fe2O3 NP) on an FTO electrode. This Fe2O3 NP-ZnO NR hybrid material functions as a nanozyme, facilitating the catalysis of cholesterol and enabling the direct transfer of electrons to the fluorine-doped tin oxide (FTO) electrode, limiting the need for costly and traditional enzymes in the detection process. This innovative non-enzymatic cholesterol biosensor showcases remarkable sensitivity, registering at 642.8 µA/mMcm2 within a linear response range of up to 9.0 mM. It also exhibits a low detection limit (LOD) of ∼12.4 µM, ensuring its capability to detect minimal concentrations of cholesterol accurately. Moreover, the developed biosensor displays exceptional selectivity by effectively distinguishing cholesterol molecules from other interfering biological species, while exhibiting outstanding stability and reproducibility. Our findings indicate that the Fe2O3 NP-ZnO NR hybrid nanostructure on the FTO electrode holds promise for enhancing biosensor stability. Furthermore, the present device fabrication platform offers versatility, as it can be adapted with various enzymes or modified with different metal oxides, potentially broadening its applicability in a wide range of biomarkers detection.

2.
ACS Omega ; 9(28): 30109-30119, 2024 Jul 16.
Artículo en Inglés | MEDLINE | ID: mdl-39035917

RESUMEN

The structural studies of the fluorinated Schiff base ligand and its copper complex were synthesized and characterized by Fourier transform infrared, UV-visible, and photoluminescence spectroscopy. Single-crystal X-ray diffraction analysis unveils a dinuclear copper complex arising from double bridging acetate anions to copper ions that are chelated by the tridentate Schiff base ligand Cu(LS). The trigonality index τ5 of 0.080 indicates a distorted square pyramidal coordination geometry for the metal. The SL ligand and complex exhibit intra- and intermolecular interactions, leading to unique supramolecular architectures. The structural changes between the free halogenated Schiff base ligand and upon coordination with the metal were extensively studied by experimental and theoretical approaches. The intra- and intermolecular interactions have been analyzed by Hirshfeld surface and quantum theory of atoms in molecules analysis, and the enrichment ratio highlights the most favored interactions in the formation of molecular packing. The chemical and physical properties, such as the HOMO - LUMO energy gap, chemical reactivity, and electron density topology, are studied using density functional theory studies. In addition, the Schiff base ligand compound is used to study the latent fingerprint analysis.

3.
ACS Omega ; 9(28): 29966-29982, 2024 Jul 16.
Artículo en Inglés | MEDLINE | ID: mdl-39035946

RESUMEN

Nanobiotechnology has ushered in a new era of scientific discovery where the unique properties of nanomaterials, such as gold nanoparticles, have been harnessed for a wide array of applications. This review explores gold nanoparticles' synthesis, properties, and multidisciplinary applications, focusing on their role as biosensors. Gold nanoparticles possess exceptional physicochemical attributes, including size-dependent optical properties, biocompatibility, and ease of functionalization, making them promising candidates for the development of biosensing platforms. The review begins by providing a comprehensive overview of gold nanoparticle synthesis techniques, highlighting the advantages and disadvantages of various approaches. It then delves into the remarkable properties that underpin their success in biosensing, such as localized surface plasmon resonance and enhanced surface area. The discussion also includes the functionalization strategies that enable specific binding to biomolecules, enhancing the sensitivity and selectivity of gold-nanoparticle-based biosensors. Furthermore, this review surveys the diverse applications of gold nanoparticles in biosensing, encompassing diagnostics, environmental monitoring, and drug delivery. The multidisciplinary nature of these applications underscores the versatility and potential of gold nanoparticles in addressing complex challenges in healthcare and environmental science. The review emphasizes the pressing need for further exploration and research in the field of nanobiotechnology, particularly regarding the synthesis, properties, and biosensing applications of gold nanoparticles. With their exceptional physicochemical attributes and versatile functionalities, gold nanoparticles present a promising avenue for addressing complex challenges in healthcare and environmental science, making it imperative to advance our understanding of their synthesis, properties, and applications for enhanced biosensing capabilities and broader scientific innovation.

4.
Anal Biochem ; 693: 115595, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-38909770

RESUMEN

Monitoring pharmaceutical drugs in various mediums is crucial to mitigate adverse effects. This study presents a chemical sensor using an oval-like zinc oxide (ZnO) nanostructure for electrochemical detection of nalbuphine. The ZnO nanostructure, produced via an efficient sol-gel technique, was extensively characterized using field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), X-ray diffraction (XRD), UV-visible spectrophotometry, and fourier transform infrared spectroscopy (FTIR). A slurry of the ZnO nanostructure in a binder was applied to a glassy carbon electrode (GCE). The sensor's responsiveness to nalbuphine was assessed using linear sweep voltammetry (LSV), achieving optimal performance by fine-tuning the pH. The sensor demonstrated a proportional response to nalbuphine concentrations up to 150.0 nM with a good regression coefficient (R2) and a detection limit of 6.20 nM (S/N ratio of 3). Selectivity was validated against various interfering substances, and efficacy was confirmed through real sample analysis, highlighting the sensor's successful application for nalbuphine detection.


Asunto(s)
Técnicas Electroquímicas , Electrodos , Nalbufina , Nanoestructuras , Óxido de Zinc , Óxido de Zinc/química , Nalbufina/análisis , Técnicas Electroquímicas/métodos , Nanoestructuras/química , Límite de Detección
5.
J Enzyme Inhib Med Chem ; 39(1): 2311818, 2024 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-38488131

RESUMEN

In this article, a new series of 2-((3,5-disubstituted-2-thioxo-imidazol-1-yl)imino)acenaphthylen-1(2H)-ones were synthesized. Imidazole-2-thione with acenaphthylen-one gave a hybrid scaffold that integrated key structural elements essential for DNA damage via direct DNA intercalation and inhibition of the topoisomerase II enzyme. All the synthesized compounds were screened to detect their DNA damage using a terbium fluorescent probe. Results demonstrated that 4-phenyl-imidazoles 5b and 5e in addition to 4-(4-chlorophenyl)imidazoles 5h and 5j would induce detectable potent damage in ctDNA. The four most potent compounds as DNA intercalators were further evaluated for their antiproliferative activity against HepG2, MCF-7 and HCT-116 utilizing the MTT assay. The highest anticancer activity was recorded with compounds 5b and 5h against the breast cancer cell line MCF-7 which were 1.5- and 3- folds more active than doxorubicin, respectively. Therefore, imidazole-2-thione tethered acenaphthylenone derivatives can be considered as promising scaffold for the development of effective dual DNA intercalators and topoisomerase II inhibitors.


Asunto(s)
Antineoplásicos , Inhibidores de Topoisomerasa II , Inhibidores de Topoisomerasa II/farmacología , Inhibidores de Topoisomerasa II/química , Relación Estructura-Actividad , Sustancias Intercalantes/farmacología , Tionas/farmacología , Antineoplásicos/farmacología , Antineoplásicos/química , Línea Celular Tumoral , Imidazoles/farmacología , ADN , Apoptosis , Simulación del Acoplamiento Molecular , ADN-Topoisomerasas de Tipo II/metabolismo , Proliferación Celular
6.
PLoS One ; 19(2): e0294286, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38386950

RESUMEN

This study highlights the effectiveness of oyster shell biocomposite for the biosorption of Cd(II) and Pb(II) ions from an aqueous solution. The aim of this work was to modify a novel biocomposite derived from oyster shell for the adsorption of Cd(II) and Pb(II) ions from aqueous solution. The studied revealed the specific surface BET surface area was 9.1476 m2/g. The elemental dispersive x-ray analysis (EDS) indicated that C, O, Ag, Ca were the predominant elements on the surface of the biocomposite after which metals ions of Cd and Pb were noticed after adsorption. The Fourier transform Irradiation (FT-IR) revealed the presence of carboxyl and hydroxyl groups on the surface. The effect of process variables on the adsorption capacity of the modified biocomposite was examined using the central composite design (CCD) of the response surface methodology (RSM). The process variables which include pH, adsorbent dose, the initial concentration and temperature were the most effective parameters influencing the uptake capacity. The optimal process conditions of these parameters were found to be pH, 5.57, adsorbent dose, 2.53 g/L, initial concentration, 46.76 mg/L and temperature 28.48°C for the biosorption of Cd(II) and Pb(II) ions from aqueous solution at a desirability coefficient of 1. The analysis of variance (ANOVA) revealed a high coefficient of determination (R2 > 0.91) and low probability coefficients for the responses (P < 0.05) which indicated the validity and aptness of the model for the biosorption of the metal ions. Experimental isotherm data fitted better to the Langmuir model and the kinetic data fitted better to the pseudo-second-order model. Maximun Cd(II) and Pb(II) adsorption capacities of the oyster shell biocomposite were 97.54 and 78.99 mg/g respectively and was obtained at pH 5.56 and 28.48°C. This investigation has provided the possibility of the utilization of alternative biocomposite as a sustainable approach for the biosorption of heavy metal ions from the wastewater stream.


Asunto(s)
Cadmio , Ostreidae , Animales , Cadmio/análisis , Espectroscopía Infrarroja por Transformada de Fourier , Adsorción , Plomo , Iones
7.
RSC Adv ; 13(46): 32786-32823, 2023 Oct 31.
Artículo en Inglés | MEDLINE | ID: mdl-37942448

RESUMEN

Spiro-heterocycles have received special attention in medicinal chemistry because of their promising biological activity. Over the years, many synthetic methodologies have been established for the construction of spirocyclic compounds. Spiro heterocycles such as spiro-azetidin-2-one, -pyrrolidine, -indol(one) and -pyran derivatives have been found to exhibit diversified biological and pharmacological activity in addition to their therapeutic properties. In view of these facts, we decided in this review to present representative synthetic approaches of the aforementioned spiro heterocycles, especially in the past 20 years.

8.
ACS Omega ; 8(15): 13492-13508, 2023 Apr 18.
Artículo en Inglés | MEDLINE | ID: mdl-37091369

RESUMEN

The clinical applications of nanotechnology are emerging as widely popular, particularly as a potential treatment approach for infectious diseases. Diseases associated with multiple drug-resistant organisms (MDROs) are a global concern of morbidity and mortality. The prevalence of infections caused by antibiotic-resistant bacterial strains has increased the urgency associated with researching and developing novel bactericidal medicines or unorthodox methods capable of combating antimicrobial resistance. Nanomaterial-based treatments are promising for treating severe bacterial infections because they bypass antibiotic resistance mechanisms. Nanomaterial-based approaches, especially those that do not rely on small-molecule antimicrobials, display potential since they can bypass drug-resistant bacteria systems. Nanoparticles (NPs) are small enough to pass through the cell membranes of pathogenic bacteria and interfere with essential molecular pathways. They can also target biofilms and eliminate infections that have proven difficult to treat. In this review, we described the antibacterial mechanisms of NPs against bacteria and the parameters involved in targeting established antibiotic resistance and biofilms. Finally, yet importantly, we talked about NPs and the various ways they can be utilized, including as delivery methods, intrinsic antimicrobials, or a mixture.

9.
Biosensors (Basel) ; 13(3)2023 Mar 12.
Artículo en Inglés | MEDLINE | ID: mdl-36979587

RESUMEN

Early-stage uric acid (UA) abnormality detection is crucial for a healthy human. With the evolution of nanoscience, metal oxide nanostructure-based sensors have become a potential candidate for health monitoring due to their low-cost, easy-to-handle, and portability. Herein, we demonstrate the synthesis of puffy balls-like cobalt oxide nanostructure using a hydrothermal method and utilize them to modify the working electrode for non-enzymatic electrochemical sensor fabrication. The non-enzymatic electrochemical sensor was utilized for UA determination using cyclic voltammetry (CV) and differential pulse voltammetry (DPV). The puffy balls-shaped cobalt oxide nanostructure-modified glassy carbon (GC) electrode exhibited excellent electro-catalytic activity during UA detection. Interestingly, when we compared the sensitivity of non-enzymatic electrochemical UA sensors, the DPV technique resulted in high sensitivity (2158 µA/mM.cm2) compared to the CV technique (sensitivity = 307 µA/mM.cm2). The developed non-enzymatic electrochemical UA sensor showed good selectivity, stability, reproducibility, and applicability in the human serum. Moreover, this study indicates that the puffy balls-shaped cobalt oxide nanostructure can be utilized as electrode material for designing (bio)sensors to detect a specific analyte.


Asunto(s)
Nanoestructuras , Ácido Úrico , Humanos , Reproducibilidad de los Resultados , Óxidos/química , Electrodos , Técnicas Electroquímicas/métodos
10.
Mol Divers ; 27(4): 1867-1878, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-36219380

RESUMEN

We herein report the facile synthesis of a series of 3,5-substituted-1,2,4-oxadiazole derivatives 9a-e and 10a-e in good to excellent yields by employing NMI-MsCl mediated amide bond formation reaction. The anti-inflammatory potential of the newly synthesized compounds were evaluated by anti-denaturation assay using diclofenac sodium as the reference drug. The compounds 9a and 9d demonstrated promising activity profile when compared to the reference standard. The SAR and molecular docking studies were also carried out for obtaining more details about the profound activity profile of the synthesized molecules. The synthesized compounds were docked against two target proteins TGF-ß and IL-1 by AutoDock vina and Auto Dock 4.2.


Asunto(s)
Antiinflamatorios , Oxadiazoles , Simulación del Acoplamiento Molecular , Estructura Molecular , Relación Estructura-Actividad , Oxadiazoles/farmacología , Oxadiazoles/química , Antiinflamatorios/farmacología , Amidas
11.
Molecules ; 27(24)2022 Dec 08.
Artículo en Inglés | MEDLINE | ID: mdl-36557818

RESUMEN

Antimicrobial resistance has posed a serious health concern worldwide, which is mainly due to the excessive use of antibiotics. In this study, gold nanoparticles synthesized from the plant Tinospora cordifolia were used against multidrug-resistant Pseudomonas aeruginosa. The active components involved in the reduction and stabilization of gold nanoparticles were revealed by gas chromatography-mass spectrophotometry(GC-MS) of the stem extract of Tinospora cordifolia. Gold nanoparticles (TG-AuNPs) were effective against P. aeruginosa at different concentrations (50,100, and 150 µg/mL). TG-AuNPs effectively reduced the pyocyanin level by 63.1% in PAO1 and by 68.7% in clinical isolates at 150 µg/mL; similarly, swarming and swimming motilities decreased by 53.1% and 53.8% for PAO1 and 66.6% and 52.8% in clinical isolates, respectively. Biofilm production was also reduced, and at a maximum concentration of 150 µg/mL of TG-AuNPs a 59.09% reduction inPAO1 and 64.7% reduction in clinical isolates were observed. Lower concentrations of TG-AuNPs (100 and 50 µg/mL) also reduced the pyocyanin, biofilm, swarming, and swimming. Phenotypically, the downregulation of exopolysaccharide secretion from P. aeruginosa due to TG-AuNPs was observed on Congo red agar plates.


Asunto(s)
Nanopartículas del Metal , Pseudomonas aeruginosa , Oro/farmacología , Piocianina/farmacología , Biopelículas , Antibacterianos/farmacología
12.
Front Chem ; 10: 1076383, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36578355

RESUMEN

Thiourea derivatives of uracil were efficiently synthesized via the reaction of 5-aminouracil with isothiocyanates. Then, we prepared uracil-containing thiazoles via condensation of thioureas with diethyl/dimethyl acetylenedicarboxylates. The structures of the products were confirmed by a combination of spectral techniques including infra-red (IR), nuclear magnetic resonance (NMR), mass spectrometry (MS) and elemental analyses. A rationale for the formation of the products is presented. The newly synthesized compounds were evaluated for their in vitro antiproliferative activity against four cancer cell lines. The compounds tested showed promising antiproliferative activity, with GI50 values ranging from 1.10 µM to 10.00 µM. Compounds 3c, 5b, 5c, 5h, 5i, and 5j were the most potent derivatives, with GI50 values ranging from 1.10 µM to 1.80 µM. Compound 5b showed potent inhibitory activity against EGFR and BRAFV600E with IC50 of 91 ± 07 and 93 ± 08 nM, respectively, indicating that this compound could serve as a dual inhibitor of EGFR and BRAFV600E with promising antiproliferative properties. Docking computations revealed the great potency of compounds 5b and 5j towards EGFR and BRAFV600E with docking scores of -8.3 and -9.7 kcal/mol and -8.2 and -9.3 kcal/mol, respectively.

13.
ACS Omega ; 7(38): 34463-34475, 2022 Sep 27.
Artículo en Inglés | MEDLINE | ID: mdl-36188271

RESUMEN

New 1,4-naphthoquinone derived by triphenylphosphaneylidene (Ph3P) and N-substituted-hydrazine-1-carbothioamides were obtained during a one-pot reaction of 2,3-dichloro-1,4-naphthoquinone with thiosemicarbazides, Ph3P and in the presence of triethyl amine (Et3N) as a catalyst. The structure of the ligands was established by ESI, IR, and NMR spectra, in addition to elemental analyses and X-ray structure analysis. On subjecting the newly prepared ligands with CuCl2 and Ph3P, autoxidation occurs, and (E)-(2-(1,4-dioxo-3-(triphenyl phosphanylidene)-3,4-dihydronaphthalen-2(1H)-ylidene)carbamothioyl)hydrazinyl)-((triphenylphosphanyl)oxy)copper derivatives were formed in very good yields. The structure of the obtained complexes was proved by ESI, IR, NMR, and UV spectra, in addition to elemental analyses and theoretical calculations.

14.
Polymers (Basel) ; 14(16)2022 Aug 17.
Artículo en Inglés | MEDLINE | ID: mdl-36015619

RESUMEN

In this work, a polypyrrole-polyethyleneimine (PPy-PEI) nano-adsorbent was successfully synthesized for the removal of methylene blue (MB) from an aqueous solution. Synthetic dyes are among the most prevalent environmental contaminants. A new conducting polymer-based adsorbent called (PPy-PEI) was successfully produced using ammonium persulfate as an oxidant. The PEI hyper-branched polymer with terminal amino groups was added to the PPy adsorbent to provide more effective chelating sites for dyes. An efficient dye removal from an aqueous solution was demonstrated using a batch equilibrium technique that included a polyethyleneimine nano-adsorbent (PPy-PEI). The best adsorption parameters were measured at a 0.35 g dosage of adsorbent at a pH of 6.2 and a contact period of 40 min at room temperature. The produced PPy-PEI nano-adsorbent has an average particle size of 25-60 nm and a BET surface area of 17 m2/g. The results revealed that PPy-PEI nano-composite was synthesized, and adsorption was accomplished in the minimum amount of time. The maximum monolayer power, qmax, for MB was calculated using the isothermal adsorption data, which matched the Langmuir isotherm model, and the kinetic adsorption data, which more closely fitted the Langmuir pseudo-second-order kinetic model. The Langmuir model was used to calculate the maximum monolayer capacity, or qmax, for MB, which was found to be 183.3 mg g-1. The as-prepared PPy-PEI nano-adsorbent totally removes the cationic dyes from the aqueous solution.

15.
Molecules ; 27(12)2022 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-35744976

RESUMEN

In this paper, we report on the design and synthesis of a novel series of quinazoline-2,4(1H,3H)-dione derivatives as fluoroquinolone-like inhibitors of bacterial gyrase and DNA topoisomerase IV to identify and develop antimicrobial agents to prevent bacterial resistance problems. Their structures were confirmed using spectroscopic analyses (IR, NMR, and EI-MS). The novel quinazoline-2,4(1H,3H)-dione derivatives were evaluated for their antimicrobial activities against Gram-positive and Gram-negative bacterial strains using the Agar well diffusion method to study the antimicrobial activities and compared them with the standard drugs. Most compounds displayed moderate activity. Among the tested compounds, the most promising compounds 13 and 15 provided broad bioactive spectrum against Gram-positive and Gram-negative strains compared to the standard drugs.


Asunto(s)
Antibacterianos , Antiinfecciosos , Antibacterianos/química , Antiinfecciosos/farmacología , Bacterias Gramnegativas , Pruebas de Sensibilidad Microbiana , Quinazolinas/química , Relación Estructura-Actividad
16.
ACS Omega ; 7(16): 13870-13877, 2022 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-35559154

RESUMEN

Clopamide (CPD, 1) is a piperidine and sulfamoylbenzamide-based diuretic drug and a potential photosensitizing sulfonamide; its phototransformation was investigated using N,N-dimethylaniline (DMA) as an electron donor and 1,4-dicyanonaphthalene (DCN) as an electron acceptor in an immersion-well-type photochemical reactor fitted with a medium-pressure mercury vapor lamp (450 W). Photodegradation of the drug Clopamide resulted in two significant products via photoinduced electron transfer. Structures of these products were deduced from their 1H NMR, 13C NMR, mass, and IR spectra. The photoproducts are 2- choloro-5-((2,6-dimethylpiperidin-1-yl)carbamoyl)benzenesulfonic acid (2) and 4-hydroxy-N-(2,6-dimethyl-1-piperidyl)-3-sulfamoyl benzamide (3). In addition to this, the comparative antioxidant potentials of the parent drug and its photoproducts were investigated using in silico molecular docking against tyrosinase in order to better understand the in vivo relevance of pharmacological action of the drug as a result of light-drug interactions. UV light has been observed to modify substituents on the benzene ring, hence loss of biological activity at the time of storage and in vivo cannot be ruled out. This suggests that Clopamide users should avoid light (natural or artificial) exposure to prevent from drug-induced photosensitivity.

17.
ACS Omega ; 7(15): 12879-12890, 2022 Apr 19.
Artículo en Inglés | MEDLINE | ID: mdl-35474844

RESUMEN

The strategies of the syntheses of various (thio)ureas, semicarbazides, thiosemicarbazides, thiazolidones, and oxadiazole derived from the [2.2]paracyclophane molecule are achieved starting with 4-(2.2]paracyclophanyl)isocyanate. The structures of the obtained products were elucidated by NMR, mass spectrometry, and infrared (IR) spectroscopy in addition to high-resolution mass spectrometry (HRMS). X-ray structure analysis was also used to prove the assigned structure.

18.
ACS Omega ; 7(51): 47869-47879, 2022 Dec 27.
Artículo en Inglés | MEDLINE | ID: mdl-36591132

RESUMEN

This research effort aims to evaluate the hazardous potential of the redox state (OH-) of zero-valent iron nanoparticles (nZVI) and its histopathological and oxidative stress toward Mozambique tilapia, Oreochromis mossambicus. X-ray powder diffraction (XRD) validated the nZVI nanoparticles' chemical composition, while transmission electron microscopy (TEM) revealed that their physical form is round and oval. The exposure to 10 g/mL of nZVI induced the activation of the cellular superoxide dismutase (SOD) activity. Dose-dependent testing of O. mossambicus had a reduction in SOD and an increase in malondialdehyde (MDA) levels, suggesting that nZVI caused oxidative damage. At a concentration of 100 g/mL, the catalase (CAT) and peroxidase (POD) activities of diverse tissues exhibited a gradual decrease after 2 days of exposure and a fast increase until day 6. The scavenging of reactive oxygen species (ROS) in the epidermis, liver, and gills of O. mossambicus deteriorated and accumulated gradually. MDA levels in the skin, gill, and liver tissues were substantially higher after 8 days of exposure to 100 and 200 g/mL nZVI compared to those of the control group and those exposed to 10 and 50 g/mL nZVI for 2 days. Extreme histological and morphological abnormalities were seen in the skin, gill, and liver tissues of experimental animals, demonstrating that the damage resulted from direct contact with nZVI in water. A one-way ANOVA followed by Dunnett's post-test was performed to investigate significant differences.

19.
Mol Divers ; 26(3): 1761-1767, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-34296385

RESUMEN

We herein report a modified methodology for the synthesis of some oxadiazoles linked to amides under mild conditions. The developed protocol using NMI-TfCl has been found to be effective and tolerant for the amide bond formation reaction of a series of electronically deactivating and sterically challenging amines. The antioxidant potential of the newly synthesized compounds has been evaluated at the later stage.


Asunto(s)
Aminas , Oxadiazoles , Amidas/química , Aminas/química , Oxadiazoles/química
20.
Mol Divers ; 26(5): 2893-2905, 2022 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-34817768

RESUMEN

We herein report the facile synthesis of a series of 3,5-substituted-1,2,4-oxadiazole derivatives in good to excellent yields. The anti-inflammatory potential of the newly synthesized compounds was evaluated by anti-denaturation assay using diclofenac sodium as the reference standard. Some of the compounds exhibited profound activity profile when compared to the standard drug. The molecular docking and SAR studies were carried out at the later stage for gaining more insights about the promising activity profile of the synthesized molecules.


Asunto(s)
Antiinflamatorios , Diclofenaco , Antiinflamatorios/farmacología , Diclofenaco/farmacología , Simulación del Acoplamiento Molecular , Estructura Molecular , Oxadiazoles/farmacología , Piperazinas , Relación Estructura-Actividad
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