SAR Analysis of New Dual Targeting Fluoroquinolones. Implications of the Benzenesulfonyl Group

M. J. NIETO; A. B. PIERINI; N. SINGH; C. R. MCCURDY; R. H. MANZO; M. R. MAZZIERI

BENTHAM SCIENCE PUBL LTD

Año: 2012

span style="LINE-HEIGHT: 115%; FONT-FAMILY: "Calibri","sans-serif"; FONT-SIZE: 11pt; mso-fareast-font-family: "Times New Roman"; mso-bidi-font-family: "Times New Roman"; mso-ansi-language: EN-US; mso-fareast-language: EN-US; mso-bidi-language: EN-US" lang="en">When a benzenesulfonyl moiety (BS) was bound to the N-piperazinyl ring of antibacterial fluoroquinolones (AMFQs) norfloxacin (NOR) or ciprofloxacin (CIP), the resulting benzenesulfonyl-fluoroquinolone (BSFQs) analogs showed an improved in vitro activity against Gram-positive strains. A bioisosterical replacement of the sulfonyl group for a carbonyl group led to the benzenecarboxamide-fluoroquinolones (BCFQs) that showed a similar trend in the antibacterial activity and spectrum. The BSFQs and BCFQs are considered members of the ?dual targeting? fluoroquinolones, targeting both DNA gyrase and topoisomerase IV. To disclose the real contribution of t