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Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-11-02 , DOI: 10.1016/j.bmcl.2020.127660 Jia Jiang 1 , Yunlei Hou 1 , Meibo Duan 1 , Baihang Wang 2 , Yachuang Wu 1 , Xiudong Ding 2 , Yanfang Zhao 1
中文翻译：
新型恶唑烷酮衍生物含氮稠合杂环部分的设计、合成及抗菌评价
更新日期：2020-12-08
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-11-02 , DOI: 10.1016/j.bmcl.2020.127660 Jia Jiang 1 , Yunlei Hou 1 , Meibo Duan 1 , Baihang Wang 2 , Yachuang Wu 1 , Xiudong Ding 2 , Yanfang Zhao 1
Affiliation
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A series of novel oxazolidinone derivatives with nitrogen-containing fused heterocyclic moiety were designed and synthesized in this article. Their antibacterial activities were measured against S. aureus, MRSA and MSSA by MIC assay. Most of them exhibited potent activity against Gram-positive pathogens comparable to Linezolid and Radezolid. Compound 3b, which exhibited significant antibacterial activity with MIC values ranging 0.5–1.0 μg/mL, might be a promising drug candidate for further investigation.
中文翻译：
新型恶唑烷酮衍生物含氮稠合杂环部分的设计、合成及抗菌评价
本文设计并合成了一系列具有含氮稠合杂环部分的新型恶唑烷酮衍生物。通过MIC法测定它们对金黄色葡萄球菌、MRSA和MSSA的抗菌活性。它们中的大多数表现出与利奈唑胺和雷德唑胺相当的对革兰氏阳性病原体的有效活性。化合物3b表现出显着的抗菌活性，MIC 值为 0.5-1.0 μg/mL，可能是进一步研究的有希望的候选药物。
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