Synthesis and antimycobacterial activity of pyrazinoic acid esters and quinolones / Síntese e atividade antimicobacteriana de ésteres do ácido pirazinóico e quinolonas

AUTOR(ES)
DATA DE PUBLICAÇÃO

2006

RESUMO

Tuberculosis affects over than one billion people around the world. Since the discovery of rifampin, in 1965, no one another important drug was introduced in therapeutics. Pyrazinamide, one of the drugs available in therapy of tuberculosis, is nowadays considered a bioprecursor of pyrazinoic acid, because resistant bacterias do not express an enzyme, pyrazinamidase, responsible by the conversion of pyrazinamide to pyrazinoic acid. Pyrazinoic acid esters exhibit antimycobacterial activity probably to better penetration through mycobacterial cell wall than the acid derivative. So, it could act in resistant strains because is activated by esterases. Some fluoroquinolones exhibit antimicobacterial activity, like ciprofloxacin, ofloxacin and levofloxacin. This work had as objective to obtain latent forms of pyrazinoic acid linking it to quinolones with antimycobacterial activity, through an ester bond, obtaining mutual prodrugs. One of the synthesized compounds showed activity in vitro, with minnimal inhibitory concentration comparable to ciprofloxacin, one of most active drugs.

ASSUNTO(S)

prodrugs pró-farmacos pyrazinoic acid Ácido pirazinóico fluoroquinolones antimicobacterial agents fluorquinolonas antimicobacterianos

ACESSO AO ARTIGO

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