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Molecules ; 23(11)2018 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-30441815

RESUMO

The one-pot synthesis of a series of pyrazoline derivatives containing the bioactive thiazole ring has been performed through a 1,3-dipolar cycloaddition reaction of N-thiocarbamoylpyrazoline and different hydrazonoyl halides or α-haloketones in the presence of DABCO (1,4-diazabicyclo[2.2.2] octane) as an eco-friendly catalyst using the solvent-drop grinding method. The structure of the synthesized compounds was elucidated using elemental and spectroscopic analyses (IR, NMR, and Mass). The activity of these compounds against human hepatocellular carcinoma cell line (HepG2) was tested and the results showed that the pyrazoline 11f, which has a fluorine substituent, is the most active. The antimicrobial activities of the newly synthesized compounds were determined against two fungi and four bacterial strains, and the results indicated that some of the newly synthesized pyrazolines are more potent than the standard drugs against test organisms.


Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Técnicas de Química Sintética , Pirazóis/síntese química , Pirazóis/farmacologia , Anti-Infecciosos/química , Antineoplásicos/química , Linhagem Celular Tumoral , Sobrevivência Celular , Humanos , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Pirazóis/química
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