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J Antibiot (Tokyo) ; 73(12): 818-827, 2020 12.
Artigo em Inglês | MEDLINE | ID: mdl-32601342

RESUMO

We report the synthesis and antimicrobial studies of a new series of naphthyl-substituted pyrazole-derived hydrazones. Many of these novel compounds are potent growth inhibitors of several strains of drug-resistant bacteria. These potent compounds have inclined growth inhibitory properties for planktonic Staphylococcus aureus and Acinetobacter baumannii, and its drug-resistant variants with minimum inhibitory concentration (MIC) as low as 0.78 and 1.56 µg ml-1, respectively. These compounds also show potent activity against S. aureus and A. baumannii biofilm formation and eradication properties. Time Kill Assay shows that these compounds are bactericidal for S. aureus and bacteriostatic for A. baumannii. The probable mode of action is the disruption of the bacterial cell membrane. Furthermore, potent compounds are nontoxic to human cell lines at several fold higher concentrations than the MICs.


Assuntos
Desenho de Fármacos , Hidrazonas/síntese química , Staphylococcus aureus/efeitos dos fármacos , Acinetobacter baumannii/efeitos dos fármacos , Biofilmes/efeitos dos fármacos , Farmacorresistência Bacteriana , Hidrazonas/farmacologia , Testes de Sensibilidade Microbiana , Naftalenos/síntese química , Naftalenos/farmacologia
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