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新型氨基/硝基取代 3-芳基香豆素类化合物的合成及构效关系研究。

Synthesis and structure-activity relationships of novel amino/nitro substituted 3-arylcoumarins as antibacterial agents.

机构信息

Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain.

出版信息

Molecules. 2013 Jan 24;18(2):1394-404. doi: 10.3390/molecules18021394.

Abstract

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.

摘要

一系列新的氨基/硝基取代的 3-芳基香豆素被合成,并评估了它们对金黄色葡萄球菌(革兰氏阳性)和大肠杆菌(革兰氏阴性)临床分离株的抗菌活性。这些分子中的一些对金黄色葡萄球菌表现出与标准药物(奥索林酸和氨苄西林)相当的抗菌活性。初步的结构-活性关系(SAR)研究表明,对金黄色葡萄球菌的抗菌活性取决于 3-芳基香豆素取代模式的位置。为了找到抗菌活性和选择性的结构特征,本研究报告了 3-芳基香豆素骨架上不同位置的硝基、甲基、甲氧基、氨基和溴取代基。

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