Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety

• Published in: Bioorganic & medicinal chemistry letters Vol. 29; no. 23; p. 126746
• Main Authors: Hou, Yunlei, Dong, Yuhong, Ye, Tianyu, Jiang, Jia, Ding, Liang, Qin, Mingze, Ding, Xiudong, Zhao, Yanfang
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 01.12.2019; Elsevier
• Subjects: Antibacterial activities; Chemistry; Chemistry, Medicinal; Chemistry, Organic; Life Sciences & Biomedicine; Linezolid; Oxazolidinone derivatives; Pharmacology & Pharmacy; Physical Sciences; Piperidinyl moiety; Science & Technology; Linezolid; Antibacterial activities; Oxazolidinone derivatives; Piperidinyl moiety; TARGET; RESISTANT; U-100592; ANTIBIOTICS; INFECTIONS; U-100766; DISCOVERY
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2019.126746

[Display omitted] In this article, a series of novel oxazolidinone derivatives containing a piperidinyl moiety was designed and synthesized. Their antibacterial activities were measured against S. aureus, MRSA, MSSA, LREF and VRE by MIC assay. Most of them exhibited potent activity against Gram-positive pathogens comparable to linezolid. Among them, compound 9h exhibited comparable activity with linezolid against human MAO-A for safety evaluation and showed moderate metabolism in human liver microsome. The most promising compound 9h, which showed remarkable antibacterial activity against S. aureus, MRSA, MSSA, LREF and VRE pathogens with MIC value of 0.25–1 μg/mL, was an interesting candidate for further investigation.