Authors: Almeida, M.V.; Saraiva, M.F.; De Souza, M.V.N.; Costa, C.F.; Vicente, F.R.C.; Lourenço, M.C.
Source: Bioorganic & Medicinal Chemistry Letters, v. 17, p. 5661-5664, 2007
Publisher: Elsevier
Abstract
Fluoroquinolone (FQ) has a broad spectrum of activity against several bacteria, mycobacteria, parasites, and other diseases. Moxifloxacin and gatifloxacin are a new generation of fluoroquinolone agents with improved activity against Gram-negative and positive bacteria. As lipophilicity is an important consideration in the design and activity of novel antibacterial agents, we report in this work the synthesis and biological evaluation of 12 lipophilic moxifloxacin or gatifloxacin derivatives, by reaction of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxoquinoline-3-carboxylic acid 13 with severals N-monoalkyl 1,2-ethanediamine or 1,3-propanediamine.Keywords: Fluoroquinolones; M. tuberculosis; Moxifloxacin; Gatifloxacin; Diamines; N-Alkyl chains; Antitubercular; Structure–activity relationships Document Type: Research Article DOI: http://dx.doi.org/10.1016/j.bmcl.2007.07.073 Publication date: 15 de Outubro de 2007
