title: Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
abstract: A series of novel gatifloxacin (GTFX) derivatives were designed, synthesized and characterized by (1)H NMR, (13)C NMR, MS and HRMS. These derivatives were evaluated for in vitro antibacterial activity against representative Gram-positive and Gram-negative strains. Our results reveal that most of the target compounds show good potency in inhibiting the growth of Staphylococcus aureus including MRSA and Staphylococcus epidermidis including MRSE. Compounds 8, 14 and 20 have useful activity against all of the tested Gram-positive and Gram-negative strains (MICs: 0.06-4 μg/mL). In particular, 20 possessing a broad antimicrobial spectrum (MICs: 0.06-1 μg/mL) was found to be 2-32-folds more potent than the reference drug levofloxacin and parent GTFX against Pseudomonas aeruginosa.
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
authors.forename: Yun
authors.initials: Y
authors.lastname: Chai
authors.forename: Ming-Liang
authors.initials: ML
authors.lastname: Liu
authors.forename: Kai
authors.initials: K
authors.lastname: Lv
authors.forename: Lian-Shun
authors.initials: LS
authors.lastname: Feng
authors.forename: Su-Jie
authors.initials: SJ
authors.lastname: Li
authors.forename: Lan-Ying
authors.initials: LY
authors.lastname: Sun
authors.forename: Shuo
authors.initials: S
authors.lastname: Wang
authors.forename: Hui-Yuan
authors.initials: HY
authors.lastname: Guo
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000077734:Gatifloxacin; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D016339:Spectrometry, Mass, Fast Atom Bombardment; D014709:Vero Cells
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D000077734:Gatifloxacin