title: Synthesis and in vitro antibacterial activity of 7-(3-amino-6,7-dihydro-2-methyl-2H-pyrazolo[4,3-c] pyridin-5(4H)-yl)fluoroquinolone derivatives.
abstract: A series of novel 7-(3-amino-6,7-dihydro-2-methyl-2H-pyrazolo[4,3-c]pyridin- 5(4H)-yl)fluoroquinolone derivatives were designed, synthesized and characterized by 1H-NMR, MS and HRMS. These fluoroquinolones were evaluated for their in vitro antibacterial activity against representative Gram-positive and Gram-negative strains. Results reveal that most of the target compounds exhibit good growth inhibitory potency against methicillin-resistant Staphylococcus epidermidis (MRSE) (MIC: 0.25-4 μg/mL) and Streptococcus pneumoniae (MIC: 0.25-1 μg/mL). In addition, compound 8f is 8-128 fold more potent than the reference drugs gemifloxacin (GM), moxifloxacin (MX), ciprofloxacin (CP) and levofloxacin (LV) against methicillin-resistant Staphylococcus aureus 10-05 and Streptococcus hemolyticus 1002 and 2-64 fold more active against methicillin-sensitive Staphylococcus aureus 10-03 and 10-04.
authors: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. wyc9999@gmail.com.
authors: Xin
authors: X
authors: Guo
authors: Ming Liang
authors: ML
authors: Liu
authors: Hui Yuan
authors: HY
authors: Guo
authors: Yu Cheng
authors: YC
authors: Wang
authors: Ju Xian
authors: JX
authors: Wang
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D015363:Quinolones