Synthesis and antitubercular activity of lipophilic moxifloxacin and gatifloxacin derivatives

被引：51
|
作者：
de Almeida, Mauro V.
Saraiva, Mauricio F.
de Souza, Marcus V. N.
da Costa, Cristiane F.
Vicente, Felipe R. C.
Lourenco, Maria C. S.
机构：
[1] Univ Fed Juiz Fora, Inst Ciencias Exatas, Dept Quim, BR-36036330 Juiz De Fora, MG, Brazil
[2] Fundacao Oswaldo Cruz, Inst Tecnol Farmacos Far Manguinhos, BR-21041250 Rio De Janeiro, Brazil
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 20期
关键词：
Fluoroquinolones; M; tuberculosis; moxifloxacin; gatifloxacin; diamines; N-alkyl chains; antitubercular; structure-activity relationships;
D O I：
10.1016/j.bmcl.2007.07.073
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：5661 / 5664
页数：4
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