Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position

Bioorganic & Medicinal Chemistry Letters
Hiroaki InagakiMakoto Takemura

Abstract

A series of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position were synthesized to obtain potent drugs for the treatment of Gram-positive infections. Some compounds exhibited excellent antibacterial activity, and potent inhibitory activity against bacterial DNA topoisomerase IV. In addition, some of the potent compounds showed reduced inhibitory activity against human DNA topoisomerase II compared with the corresponding noncyclopropane-fused compounds.

References

Mar 1, 1982·Antimicrobial Agents and Chemotherapy·M H Cynamon, P A Granato
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Mar 20, 1999·Chest·T M File

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Citations

Mar 11, 2008·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Alireza ForoumadiAbbas Shafiee
May 18, 2007·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Abbas PardakhtyMahmoud Reza Heidari
Oct 31, 2012·Chemistry : a European Journal·Emilie DavidXavier Pannecoucke
Oct 14, 2008·Expert Review of Anti-infective Therapy·Michael R Jacobs

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