INVESTIGADORES
ALOVERO Fabiana De Lujan
artículos
Título:
A new class of fluoroquinolone: Benzennesulfonamidefluoroquinolones (BSFQs). Antibacterial Activity and SAR studies
Autor/es:
MARCELO J, NIETO; FABIANA L. ALOVERO Ó F. L. ALOVERO; RUBEN HILARIO, MANZO; MARÍA ROSA, MAZZIERI
Revista:
EUROPEAN JOURNAL OF MEDICAL CHEMISTRY
Editorial:
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Referencias:
Lugar: Paris; Año: 1999 vol. 34 p. 209 - 214
ISSN:
0223-5234
Resumen:
N-Sulfanilylnorfloxacin was chosen as lead compound to develop a new series of benzenesulfonamidefluoroquinolones (BSFQs). Eight new compounds with different p-substituents on the phenyl group were prepared and their in vitro antibacterial activities were evaluated. The presence of the benzenesulfonylamido groups (BS) bound to the piperazinyl ring shifted the activity of classic antimicrobial fluoroquinolones from being more active against Gram negative to Gram positive strains. Analogs with p-NHCH3, p-H or p-NO2 were more active than norfloxacin. QSAR studies through Hansch analysis showed a linear correlation of the activity with electronic distribution (empirical descriptors) along with Sterimol parameters. Small electron?donor groups with hydrophilic properties increase the in vitro activity against Gram positive bacteria.
