INFIQC   05475
INSTITUTO DE INVESTIGACIONES EN FISICO- QUIMICA DE CORDOBA
Unidad Ejecutora - UE
congresos y reuniones científicas
Título:
Synthesis and antimicrobial activity of hydrothiazine, hydrooxazine, hydroquinazolinone and hydropyrimidine derivatives
Autor/es:
FAILLACE, M. S.; BRITO, M. R. M.; PEPINO, A. J.; ; COSTA, J. P.; SILVA, A. P. S. C. L.; PACHECO, A. G. M.; ALMEIDA, J. R. G. S.; ARGÜELLO, G. A.; ; FREITAS, R. M.; PELÁEZ, W. J.
Lugar:
Córdoba
Reunión:
Congreso; 2014 Reunión Internacional de Ciencias Farmacéuticas RICIFA; 2014
Institución organizadora:
Universidad Nacional de Córdoba-Depto de Farmacia.
Resumen:
We present here the synthesis, purification and structural determination of nine hexahydro compounds. Their syntheses were performed in solution resulting in all cases very good yields. Furthermore, the antimicrobial activity was evaluated using the following bacterial strains: ATCC Bacillus cereus, Enterococcus faecalis, Escherichia coli, Klebsiella pneumoniae, Salmone laenterica, Serratia marcescens, S. flexneri and Staphylococcus aureus. These baterial strains were obtained from the ?Instituto Nacional de Controle de Qualidade em Saúde? (INCQS/FIOCRUZ, Brasil). The measurement of the antibacterial effect was performed according to the Clinical Laboratory Standards. All compounds were tested in the concentration range 500-3.91 µg/mL. The same methodology was employed for the positive control (gentamicin -1.6 mg/mL). The parameters analyzed were the minimum inhibitory concentration (MIC) and the minimun bactericidal concentration (MBC). The results were significative as the nine compounds present positive activity (WP2 MIC= 15,62; WP6 MIC= 500; WP33 MIC= 500; WP45 MIC= 125; WP50 MIC= 500; WP55 MIC= 31,25; WP78 MIC= 250; WP2331 MIC= 3,91; WP2332 MIC= 31,25) and six of them demostrated bactericidal activity (WP2 MCB= 125; WP45 MCB= 500; WP55 MCB= 62,5; WP78 MCB= 500; WP2331 MCB= 31,25; WP2332 MCB= 62,5). WP2331 presents the lowest inhibitory and bactericidal concentration (3.91 and 31.25 µg/mL, respectively). Compound groups: WP2 and WP6 are hexahidroquinazolines; WP33 and WP78 are hexahydropyrimidines; WP45, WP50, WP2331 and WP2332 are hexahydrooxazines while WP55 is an hexahydrothiazine. Key-words: hexahydroquinazolinones, antimicobacterial; inhibitory concentration.