Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety

• Published in: Bioorganic & medicinal chemistry letters Vol. 32; p. 127660
• Main Authors: Jiang, Jia, Hou, Yunlei, Duan, Meibo, Wang, Baihang, Wu, Yachuang, Ding, Xiudong, Zhao, Yanfang
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 15.01.2021; Elsevier
• Subjects: Antibacterial activities; Chemistry; Chemistry, Medicinal; Chemistry, Organic; Gram-positive bacteria; Life Sciences & Biomedicine; Nitrogen-containing fused heterocyclic moiety; Oxazolidinone derivatives; Pharmacology & Pharmacy; Physical Sciences; Science & Technology; Gram-positive bacteria; Antibacterial activities; Nitrogen-containing fused heterocyclic moiety; Oxazolidinone derivatives; TARGET; ANTIBIOTICS; ANALOGS; RESISTANCE
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2020.127660

[Display omitted] 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.