Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 20, Pages 5661-5664Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.07.073
Keywords
Fluoroquinolones; M. tuberculosis; moxifloxacin; gatifloxacin; diamines; N-alkyl chains; antitubercular; structure-activity relationships
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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-cyclo-propyl-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. (c) 2007 Elsevier Ltd. All rights reserved.
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