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药学学报  2015 

新型截短侧耳素衍生物的合成及抗菌活性研究

, PP. 1297-1304

Keywords: 截短侧耳素衍生物,抗菌活性,含氮杂环化合物,耐药的革兰阳性病原体

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Abstract:

通过将含氮杂环与wl001的2-氨基噻唑侧链相连,设计合成了一系列新的截短侧耳素衍生物。用革兰阳性和革兰阴性菌对该系列化合物进行体外抗菌活性测定,合成的大多数化合物不仅在药物敏感菌株中表现出抗菌活性,而且在耐药菌株中也有相同效果。特别值得注意的是具有饱和氮杂环的化合物表现出显著的抗菌活性(0.0625~8μg·ml-1),优于或类似于阿莫西林、泰妙菌素和左氧氟沙星。此外,15a和15b含有哌啶或吗啉的化合物同样能够有效的抑制革兰阴性菌。本研究为相关截短侧耳素衍生物的设计提供了一个新视野,为进一步研究治疗耐药性致病菌奠定了基础。

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