title: Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
abstract: A series of C10 non-basic building block-substituted, levofloxacin core-based derivatives were synthesized in 43-86% yield. The antibacterial activity of these new fluoroquinolones was evaluated using a standard broth microdilution technique. The quinolone (S)-9-fluoro-10-(4-hydroxypiperidin-1-yl)-3-methyl-7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid L-arginine tetrahydrate exhibited superior antibacterial activity against quinolone-susceptible and resistant strains compared with the clinically used fluoroquinolones ciprofloxacin, levofloxacin, moxifloxacin, penicillin, and vancomycin, especially to the methicillin-resistant Staphylococcus aureus clinical isolates, penicillin-resistant Streptococcus pneumoniae clinical isolates, and Streptococcus pyogenes.
authors.affiliation: Department of Medicinal Chemistry, Guangzhou Baiyunshan Pharmaceutical General Factory, Guangzhou 510515, China. Electronic address: 200315@byszc.com.
authors.forename: Xiaoguang
authors.initials: X
authors.lastname: Huang
authors.affiliation: Department of Medicinal Chemistry, Guangzhou Baiyunshan Pharmaceutical General Factory, Guangzhou 510515, China.
authors.forename: Yingxia
authors.initials: Y
authors.lastname: Bao
authors.affiliation: Department of Medicinal Chemistry, Guangzhou Baiyunshan Pharmaceutical General Factory, Guangzhou 510515, China.
authors.forename: Shaoxuan
authors.initials: S
authors.lastname: Zhu
authors.affiliation: Department of Medicinal Chemistry, Guangzhou Baiyunshan Pharmaceutical General Factory, Guangzhou 510515, China.
authors.forename: Xiaona
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Department of Medicinal Chemistry, Guangzhou Baiyunshan Pharmaceutical General Factory, Guangzhou 510515, China.
authors.forename: Shilong
authors.initials: S
authors.lastname: Lan
authors.affiliation: Department of Medicinal Chemistry, Guangzhou Baiyunshan Pharmaceutical General Factory, Guangzhou 510515, China.
authors.forename: Ting
authors.initials: T
authors.lastname: Wang
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D064704:Levofloxacin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010403:Penicillin Resistance / Q000187:drug effects; D013296:Streptococcus pneumoniae / Q000187:drug effects*; D013297:Streptococcus pyogenes / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D064704:Levofloxacin
keywords: Levofloxacin core; Methicillin-resistant Staphylococcus aureus; Non-basic building blocks; Penicillin-resistant Streptococcus pneumoniae; Streptococcus pyogenes