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1.
Int J Surg ; 97: 106204, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34974199

RESUMO

Coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has resulted in a catastrophic pandemic and severely impacted people's livelihoods worldwide. In addition, the emergence of SARS-CoV-2 variants has posed a severe threat to humankind. Due to the dearth of therapeutic options during the commencement of the pandemic, convalescent plasma therapy (CPT) played a significant part in the management of patients with severe form of COVID-19. Several recent studies have proposed various protective effects of CPT, such as antiviral, anti-inflammatory, anti-thrombotic, and immunomodulatory actions, curtailing the devastating consequences of the SARS-CoV-2 infection. On the contrary, several clinical studies have raised some serious concerns about the effectiveness and reliability of CPT in the management of patients with COVID-19. The protective effects of CPT in severely ill patients are yet to be proved. Moreover, the emergence of SARS-CoV-2 variants has raised concerns about the effectiveness of CPT against COVID-19. Therefore, to establish concrete evidence of the efficacy of CPT and adjudicate its inclusion in the management of COVID-19, an updated review of present literature is required, which could help in the development of an efficient therapeutic regimen to treat COVID-19 amid the emergence of new viral variants.


Assuntos
COVID-19 , SARS-CoV-2 , COVID-19/terapia , Humanos , Imunização Passiva , Reprodutibilidade dos Testes , Soroterapia para COVID-19
2.
Bioorg Med Chem Lett ; 21(8): 2547-9, 2011 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-21396814

RESUMO

A series of 4-styrylcoumarin have been synthesized by Knoevenagel condensation between substituted 4-methylcoumarin-3-carbonitrile and different heterocyclic or aromatic aldehydes. 4-Methylcoumarin-3-carbonitrile has been synthesized by the base catalyzed reaction between substituted 2-hydroxyacetophenone and ethyl cyanoacetate. The structures of the newly synthesized compounds were confirmed by (1)H NMR, IR and mass spectral analysis. All the compounds were evaluated for their anti-inflammatory activity (against TNF-α and IL-6) and anti-tubercular activity. Compounds 6a, 6h and 6j exhibited promising activity against IL-6 with 72-87% inhibition and compound 6v showed potent activity against TNF-α with 73% inhibition at 10 µM concentration. Whereas compounds 6n, 6o, 6r and 6u showed very good anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain at <6.25 µM.


Assuntos
Anti-Inflamatórios/síntese química , Antituberculosos/síntese química , Cumarínicos/química , Interleucina-6/antagonistas & inibidores , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antituberculosos/química , Antituberculosos/farmacologia , Cumarínicos/síntese química , Cumarínicos/farmacologia , Interleucina-6/metabolismo , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos , Fator de Necrose Tumoral alfa/metabolismo
3.
Bioorg Med Chem Lett ; 21(11): 3443-6, 2011 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-21515046

RESUMO

A series of novel N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives has been synthesized. All the newly synthesized compounds were evaluated for their anti-HIV activity using MTT method. Most of these compounds showed moderate to potent activity against wild-type HIV-1 with an EC(50) ranging from >7 EC(50) [µg/ml] to <100 EC(50) [µg/ml]. Among them, N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide 6v was identified as the most promising compound (EC(50)=<7 µg/ml). Among all the compounds, three compounds 6m, 6v and 6u have been exhibits potent anti-HIV activity against MT-4 cells.


Assuntos
Acetamidas/síntese química , Acetamidas/farmacologia , Antirretrovirais/síntese química , Antirretrovirais/farmacologia , HIV-1/efeitos dos fármacos , Acetamidas/química , Antirretrovirais/química , Benzopiranos/síntese química , Benzopiranos/química , Benzopiranos/farmacologia , Benzotiazóis/síntese química , Benzotiazóis/química , Benzotiazóis/farmacologia , Células Cultivadas , Humanos , Estrutura Molecular
4.
Eur J Med Chem ; 46(5): 1942-8, 2011 May.
Artigo em Inglês | MEDLINE | ID: mdl-21396744

RESUMO

A new series of benzofuran-2-yl(4,5-diydro-3,5-substituted diphenylpyrazol-1-yl) methanone derivatives 8a-x by the reaction of the benzofuran-2-carbohydrazides 7 with various chalcone derivatives 3a-x using microwave irradiation has been described. The effect of synthesized compounds 8a-v was studied against human cancer cell lines for their antiproliferative activity and reversal of multidrug resistance on human MDR1-gene transfected mouse lymphoma cells. Among the 24 compounds, the 8c and 8h showed good antiproliferative activity 8b, 8f and 8k were exhibited good MDR reversal activity. The main significance of the process is easy workup process, short reaction time and high yield of the new compounds for biological interest. However, the studies on genetically modified multidrug resistant cancer cells are costly and time consuming.


Assuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/genética , Antineoplásicos/farmacologia , Benzofuranos/farmacologia , Resistência a Múltiplos Medicamentos , Resistencia a Medicamentos Antineoplásicos , Linfoma de Células T/tratamento farmacológico , Metano/farmacologia , Subfamília B de Transportador de Cassetes de Ligação de ATP , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Benzofuranos/síntese química , Benzofuranos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Linfoma de Células T/genética , Linfoma de Células T/patologia , Metano/análogos & derivados , Metano/química , Camundongos , Estrutura Molecular , Relação Quantitativa Estrutura-Atividade , Estereoisomerismo , Relação Estrutura-Atividade , Transfecção
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