RESUMO
With the goal of discovering new anti-infective agents active against microbial biofilms, this investigation focused on some natural pyrrolomycins, a family of halogenated pyrrole antibiotics. In this study the anti-staphylococcal biofilm activity of pyrrolomycins C, D, F1, F2a, F2b, F3 and of the synthesized related compounds I, II, III were investigated. The susceptibility of six staphylococcal biofilms was determined by methyltiazotetrazolium staining. Most of the compounds were active at concentrations of 1.5 microg ml(-1) with significant inhibition percentages. A few of the compounds were active at the lowest screening concentration of 0.045 microg ml(-1). The population log reduction of activity against the two best biofilm forming Staphylococcus aureus strains as determined by viable plate counts is also reported. In order to adequately assess the utility of these compounds, their toxicity against human cells was evaluated. It is concluded that pyrrolomycins and synthetic derivatives are promising compounds for developing novel effective chemical countermeasures against staphylococcal biofilms.
Assuntos
Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Pirróis/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus epidermidis/efeitos dos fármacos , Antibacterianos/química , Aderência Bacteriana/efeitos dos fármacos , Aderência Bacteriana/genética , Biofilmes/crescimento & desenvolvimento , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Estrutura Molecular , Reação em Cadeia da Polimerase , Pirróis/química , Pirróis/toxicidade , Staphylococcus aureus/genética , Staphylococcus aureus/fisiologia , Staphylococcus epidermidis/genética , Staphylococcus epidermidis/fisiologiaRESUMO
The synthesis and antimicrobial activity of new pyrrole derivatives structurally related to monodeoxypyoluteorin are described. The insertion of a keto or methylene spacer between the phenol group and the pyrroloyl moiety of brominated 2-(2'-hydroxybenzoyl)pyrroles leads to a decrease of the antibacterial activity.
