Synthesis of New 3-(2-Chloroquinolin-3-yl)-5-Phenylisoxazole Derivatives via Click-Chemistry Approach

被引:10
|
作者
Fernandez-Galleguillos, Carlos [1 ]
Saavedra, Luis A. [1 ]
Gutierrez, Margarita [1 ]
机构
[1] Univ Talca, Inst Quim Recursos Nat, Lab Sintesis Organ, Talca 3460000, Chile
关键词
quinoline; isoxazol; 1,3-dipolar cycloaddition; click chemistry; IN-VITRO; LIBRARY; BINDING; AZOLES; DRUG;
D O I
10.5935/0103-5053.20140002
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Herein, we report the synthesis of new substituted 3-(2-chloroquinolin-3-yl)-5-phenylisoxazole (3a-j) by click chemistry in good to moderate yields. This approach is based on the regioselective copper(I)-catalyzed cycloaddition between different nitrile oxides derived from 2-chloroquinoline-3- carbaldehyde (2a-j) and phenylacetylene. Finally these derivatives were screened for their antibacterial evaluation in vitro against three Gram-negative clinical bacteria: Escherichia coli, Pseudomonas aeruginosa and Acinetobacter baumannii using standard methods.
引用
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页码:365 / 371
页数:7
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