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Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation

Authors
  • Sadowski, Elodie
  • Bercot, Beatrice
  • Chauffour, Aurélie
  • Gomez, Catherine
  • Varon, Emmanuelle
  • Mainardis, Mary
  • Sougakoff, Wladimir
  • Mayer, Claudine
  • Sachon, Emmanuelle
  • Anquetin, Guillaume
  • Aubry, Alexandra
Publication Date
Jan 01, 2022
Identifiers
DOI: 10.1016/j.bmcl.2021.128450
PMID: 34774742
OAI: oai:HAL:hal-03448562v2
Source
HAL
Keywords
Language
English
License
Unknown
External links

Abstract

This paper reports on the design of a series of 10 novel lipophilic piperazinyl derivatives of the 1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, their synthesis, their characterisation by 1H, 13C and 19F NMR, IR spectroscopy and HRMS, as well as their biological activity against bacteria of medical interest. Among these derivatives, 2 were as potent as the parent quinolone against Neisseriagonorrhoeae whereas all the compounds displayed lower activity than the parent quinolone against other bacteria of medical interest. Our results showing that the increased lipophilicity was deleterious for antibacterial activity may help to design new quinolone derivatives in the future, especially lipophilic quinolones which have been poorly investigated previously.

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