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J Enzyme Inhib Med Chem ; 31(sup2): 104-110, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27319400

RESUMO

A set of novel quinolone-triazole conjugates (12-31) were synthesized in three steps in good yields starting from 2-phenylquinoline-4-carboxylic acid. All the intermediates, as well as the final 1,2,4-triazolyl quinolines were fully characterized by their detailed spectral analysis utilizing different techniques such as IR, 1H NMR, 13C NMR, and finally mass spectrometry. All the synthesized compounds were evaluated in vitro for their potential antibacterial activity and their preliminary safety profile was assessed through cytotoxicity assay. Additionally, six selected conjugates were evaluated for their antioxidative properties on the basis of density functional theory calculations, using radical scavenging assay (DPPH) and cellular antioxidant assay. The reported results encourage further investigation of selected compounds and are shading light on their potential pharmacological use.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Quinolinas/química , Quinolinas/farmacologia , Triazóis/farmacologia , Antibacterianos/síntese química , Antioxidantes/síntese química , Antioxidantes/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Teoria Quântica , Quinolinas/síntese química , Relação Estrutura-Atividade , Triazóis/química
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