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1.
Chem Biodivers ; 20(7): e202300482, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37220245

RESUMO

Prodrugs of dexibuprofen having ester moieties instead of free carboxylic acid which involves in gastrointestinal side effects have been synthesized. Dexibuprofen acid was condensed with different alcohols/phenols to afford the ester prodrugs. All of the synthesized prodrugs were characterized by their physical attributes, elemental analysis, FT-IR, 1 H-NMR, and 13 C-NMR spectroscopy. The in vitro anti-inflammatory studies was done by chemiluminescence technique reflect prodrugs have been more potent, owing to the different chemical structures. Lipoxygenase enzyme inhibition assay was also assess and found compound DR7 with IC50 =19.8 µM), DR9 (IC50 =24.8 µM) and DR3 (IC50 =47.2 µM) as compared with Dexibuprofen (IC50 =156.6 µM). It was also evaluated for docking studies revealed that DR7 has found to be more potent anti-inflammatory against 5-LOX (3 V99) as well as analgesic against COX-II (5KIR) enzyme. Anti-oxidant activities were also performed, DR3 (86.9 %), DR5 (83.5 %), DR7 (93.9 %) and DR9 (87.4 %) were found to be more anti-oxidant as compared to (2S)-2-[4-(2-methylpropyl)phenyl]propanoic acid (52.7 %).


Assuntos
Antioxidantes , Pró-Fármacos , Antioxidantes/farmacologia , Simulação de Acoplamento Molecular , Espectroscopia de Infravermelho com Transformada de Fourier , Anti-Inflamatórios/farmacologia , Ésteres , Estrutura Molecular , Relação Estrutura-Atividade
2.
Ecotoxicol Environ Saf ; 210: 111834, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33401200

RESUMO

An attempt has been made in correspondence to explain the consequences of chemical pollution after the explosion of ammonium nitrate (AN) in Beirut (capital of Lebanon). The effects of chemicals in the air, soil, and water have been discussed. In addition, the study emphasizes on the research to restore the environment and enhanced safety measurements.


Assuntos
Vazamento de Resíduos Químicos , Desastres , Explosões , Nitratos/toxicidade , Animais , Meio Ambiente , Humanos , Líbano , Risco
3.
Org Lett ; 22(9): 3519-3523, 2020 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-32301619

RESUMO

Cobalt-catalyzed highly branched- and enantioselective allylic alkylation of malononitriles has been developed. Chiral γ,δ-unsaturated malononitriles could be synthesized with >20:1 branched/linear regioselectivity and up to 99% enantiomeric excess from easily accessible racemic allylic carbonates under mild reaction conditions. The electron-rich and sterically less hindered bisoxazolinephosphine ligand is essential to realize the high reactivity in the carbon-carbon bond formation process.

4.
J Colloid Interface Sci ; 574: 87-96, 2020 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-32305731

RESUMO

Due to the high electromagnetic interference (EMI) pollution, electromagnetic wave (EMW) absorption materials have risen as an important research area in material science and technology. Herein, the prepared carbonized ZIF-67 (CZIF) nanocomposites with polypyrrole (PPy) showed significantly enhanced electromagnetic wave absorption performance. The CZIF-PPy nanocomposites were prepared by the solvothermal and in-situ polymerization method. The CZIF-PPy nanocomposites possess a decent reflection loss (RL) value between the 2-18 GHz frequency range. The enhanced surface properties and magnetic-dielectric interfacial polarization plays an important role to achieve higher reflection loss and broader absorption bandwidth. This work explains the importance of magnetic-dielectric interface and may lead to design of more advanced hybrid electromagnetic wave absorption systems.

5.
Nanoscale Res Lett ; 13(1): 158, 2018 May 21.
Artigo em Inglês | MEDLINE | ID: mdl-29785568

RESUMO

In this paper, we provide a detailed insight on InGaAs/InAlAs separate absorption, grading, charge, and multiplication avalanche photodiodes (SAGCM APDs) and a theoretical model of APDs is built. Through theoretical analysis and two-dimensional (2D) simulation, the influence of charge layer and tunneling effect on the APDs is fully understood. The design of charge layer (including doping level and thickness) can be calculated by our predictive model for different multiplication thickness. We find that as the thickness of charge layer increases, the suitable doping level range in charge layer decreases. Compared to thinner charge layer, performance of APD varies significantly via several percent deviations of doping concentrations in thicker charge layer. Moreover, the generation rate (G btt ) of band-to-band tunnel is calculated, and the influence of tunneling effect on avalanche field was analyzed. We confirm that avalanche field and multiplication factor (M n ) in multiplication will decrease by the tunneling effect. The theoretical model and analysis are based on InGaAs/InAlAs APD; however, they are applicable to other APD material systems as well.

6.
Drug Res (Stuttg) ; 67(10): 596-605, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28672409

RESUMO

A series of acylthioureas was synthesized and their inhibitory effects on the DPPH and jack bean urease were evaluated. The results showed that all of the synthesized compounds exhibited significant jack bean urease inhibitory activities. Especially, 1-(4-chlorophenyl)-3 palmitoylthiourea 5a bearing 4-chloro substituted phenyl ring exhibited the most potent tyrosinase inhibitory activity with an IC50 value 0.0170 µM compared to the IC50 value of 4.720 µM of thiourea used as standard. The inhibition mechanism analyzed by Lineweaver-Burk plots revealed that the type of inhibition of compound 5a on tyrosinase was noncompetitive. The docking study against jack bean urease enzyme was also performed to determine the binding affinity of the compounds. The compounds 4c and 4e showed the highest binding affinity with the active binding site of tyrosinase. The initial structure activity relationships (SARs) analysis suggested that further development of such compounds might be of interest. The statistics of our results endorses that all compounds and particularly 5a may serve as a structural template for the design and development of novel urease inhibitors Graphical Abstract.


Assuntos
Inibidores Enzimáticos/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Ácido Palmítico/química , Tioureia/química , Urease/antagonistas & inibidores , Cinética , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase/química , Ácido Palmítico/metabolismo , Relação Estrutura-Atividade , Urease/metabolismo
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