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

Molecules. 2011 Mar 22;16(3):2626-35. doi: 10.3390/molecules16032626.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Quinolones / chemical synthesis*
  • Quinolones / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Quinolones