Synthesis and Structure-Activity Relationships of Novel Amino/Nitro Substituted 3-Arylcoumarins as Antibacterial Agents

被引:65
|
作者
Matos, Maria J. [1 ]
Vazquez-Rodriguez, Saleta [1 ]
Santana, Lourdes [1 ]
Uriarte, Eugenio [1 ]
Fuentes-Edfuf, Cristina [2 ]
Santos, Ysabel [2 ]
Munoz-Crego, Angeles [2 ]
机构
[1] Univ Santiago de Compostela, Dept Quim Organ, Fac Farm, Santiago De Compostela 15782, Spain
[2] Univ Santiago de Compostela, Fac Biol, Dept Microbiol & Parasitol, Santiago De Compostela 15782, Spain
来源
MOLECULES | 2013年 / 18卷 / 02期
关键词
amino/nitro substituted 3-arylcoumarins; Perkin reaction; antibacterial assays; S; aureus; E; coli; ANTIMICROBIAL ACTIVITY; MEDICINAL CHEMISTRY; SIMPLE COUMARINS; DNA GYRASE; POTENT; 3-PHENYLCOUMARINS; INHIBITORS; DISCOVERY; ANALOGS; SERIES;
D O I
10.3390/molecules18021394
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A new series of amino/nitro-substituted 3-arylcoumarins were synthesized and their antibacterial activity against clinical isolates of Staphylococcus aureus (Gram-positive) and Escherichia coli (Gram-negative) was evaluated. Some of these molecules exhibited antibacterial activity against S. aureus comparable to the standards used (oxolinic acid and ampicillin). The preliminary structure-activity relationship (SAR) study showed that the antibacterial activity against S. aureus depends on the position of the 3-arylcoumarin substitution pattern. With the aim of finding the structural features for the antibacterial activity and selectivity, in the present manuscript different positions of nitro, methyl, methoxy, amino and bromo substituents on the 3-arylcoumarin scaffold were reported.
引用
收藏
页码:1394 / 1404
页数:11
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