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Acta Chim Slov ; 67(4): 1139-1147, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33533467

RESUMO

1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone derivatives. The structures of compounds were characterized by IR, 1H NMR spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory activity using lipoxygenase inhibitory method and antidiabetic activity using the ?-glucosidase inhibitory method. Especially, pyrazoline derivatives exhibited stronger anti-inflammatory activity than the reference drug indomethacin (IC50: 50.45 µM) and their IC50 values were in the range of 0.68 and 4.45 µM. In addition, the ADME properties of all chalcone and pyrazoline derivatives were calculated by Lipinski's and Veber's rules.


Assuntos
Sequestradores de Radicais Livres/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Lipoxigenase/farmacologia , Pirazóis/farmacologia , Chalconas/síntese química , Desenho de Fármacos , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/farmacocinética , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/farmacocinética , Inibidores de Lipoxigenase/síntese química , Inibidores de Lipoxigenase/farmacocinética , Pirazóis/síntese química , Pirazóis/farmacocinética , Saccharomyces cerevisiae/enzimologia , Proteínas de Saccharomyces cerevisiae/antagonistas & inibidores
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