期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 20, 页码 5661-5664出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.07.073
关键词
Fluoroquinolones; M. tuberculosis; moxifloxacin; gatifloxacin; diamines; N-alkyl chains; antitubercular; structure-activity relationships
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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