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1.
Molecules ; 26(12)2021 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-34207756

RESUMO

Since December 2019, humanity has faced an important global threat. Many studies have been published on the origin, structure, and mechanism of action of the SARS-CoV-2 virus and the treatment of its disease. The priority of scientists all over the world has been to direct their time to research this subject. In this review, we highlight chemical studies and therapeutic approaches to overcome COVID-19 with seven different sections. These sections are the structure and mechanism of action of SARS-CoV-2, immunotherapy and vaccine, computer-aided drug design, repurposing therapeutics for COVID-19, synthesis of new molecular structures against COVID-19, food safety/security and functional food components, and potential natural products against COVID-19. In this work, we aimed to screen all the newly synthesized compounds, repurposing chemicals covering antiviral, anti-inflammatory, antibacterial, antiparasitic, anticancer, antipsychotic, and antihistamine compounds against COVID-19. We also highlight computer-aided approaches to develop an anti-COVID-19 molecule. We explain that some phytochemicals and dietary supplements have been identified as antiviral bioproducts, which have almost been successfully tested against COVID-19. In addition, we present immunotherapy types, targets, immunotherapy and inflammation/mutations of the virus, immune response, and vaccine issues.


Assuntos
COVID-19/prevenção & controle , Antivirais/química , Antivirais/uso terapêutico , Produtos Biológicos/uso terapêutico , COVID-19/patologia , COVID-19/terapia , COVID-19/virologia , Vacinas contra COVID-19/administração & dosagem , Vacinas contra COVID-19/imunologia , Síndrome da Liberação de Citocina/prevenção & controle , Desenho de Fármacos , Reposicionamento de Medicamentos , Humanos , Imunoterapia , SARS-CoV-2/genética , SARS-CoV-2/isolamento & purificação , SARS-CoV-2/fisiologia
2.
Drug Chem Toxicol ; 44(6): 595-600, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31621427

RESUMO

In a previous study, 3-amino-4-[4-(dimethylamino)phenyl]-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxide (DPTD), which is five-membered cyclosulfamide, was synthesized and structurally characterized. The aim of this study was to investigate the cytotoxic and genotoxic effects of DPTD on cultured human lymphocytes in the presence and absence of a metabolic activation system (S9 mix). The cytotoxicity and genotoxicity of DPTD in human peripheral blood lymphocytes were examined in vitro by using chromosomal aberration (CA) and micronucleus (MN) tests. Mitomycin-C (MMC) for cultures without S9 mix and cyclophosphamide monohydrate (CP) for cultures with S9 mix were used as positive controls. The cultures were treated with DPTD (45, 90, and 180 µg/mL) in the absence and presence of S9 mix. The cells were also co-treated with DPTD together with MMC or CP. DPTD showed cytotoxic activity due to decreases in mitotic index (MI) and nuclear division index (NDI) in the absence and presence of S9 mix. DPTD also increased the CAs, aberrant cells with CAs and MN values in cultures with and without S9 mix. When DPTD and MMC or CP were used together, lower MI and NDI values and higher CA and MN values were found than those DPTD treated alone. Both DPTD and its metabolites have cytotoxic, cytostatic and genotoxic potential on human peripheral blood lymphocyte cultures under the experimental conditions. Furthermore, co-treatment of DPTD and MMC or CP can cause more cytotoxicity and genotoxicity. Our results indicated that the use of DPTD with other chemotherapeutic drugs may display more effective results.


Assuntos
Mutagênicos , Tiadiazóis , Células Cultivadas , Aberrações Cromossômicas , Humanos , Linfócitos , Testes para Micronúcleos , Índice Mitótico , Mutagênicos/toxicidade , Troca de Cromátide Irmã , Tiadiazóis/toxicidade
3.
Molecules ; 25(4)2020 Feb 18.
Artigo em Inglês | MEDLINE | ID: mdl-32085429

RESUMO

In this paper, a series of new substituted-5-pyrazolones were first synthesized, then formulated by the Vilsmeier-Haack reaction to obtain substituted-4-carbaldehyde-5-pyrazolones. In the final step, when urea was reacted with formulated pyrazolones, we found that, instead of the C=N bond in azomethine form, the compounds tautomerized to form a series of novel pyrazole-4-ylidenemethylurea structures. The structures of these compounds were elucidated by FTIR, 1H, 13C NMR, LC-MS/MS, and elemental analysis methods. The cytotoxic and antioxidant effects of substituted 5-pyrazolones and their pyrazolone-urea derivatives were investigated in metastatic A431 and noncancerous HaCaT human keratinocytes by a mitochondrial activity test. The effects of the compounds on the migration of cancerous and noncancerous cell lines were investigated by using a cell scratch assay. The General Linear Model, Statistical Package for Social Sciences (SPSS v26) was used to determine if there was a statistically significant difference between the control and the treatment groups. Four of the nine compounds showed an antioxidant effect. All 5-pyrazolone-urea compounds showed higher toxicity (p < 0.05) in cancerous A431 cells compared to noncancerous cells at all time points. All compounds also showed a biphasic hormetic effect. Four of the nine compounds inhibited cell migration.


Assuntos
Pirazolonas/síntese química , Ureia/síntese química , Linhagem Celular , Ensaios de Migração Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Peróxido de Hidrogênio/toxicidade , Espectroscopia de Prótons por Ressonância Magnética , Pirazolonas/química , Pirazolonas/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Estereoisomerismo , Ureia/química
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