The simple synthesis and antimicrobial activity of novel fluoroquinolone derivatives from natural amino acid salts

Abstract

A simple synthetic route was developed to prepare novel fluoroquinolone derivatives from amino acid salts. A facile route preparing the quinolone intermediates in one pot was explored which can facilitate the industrial operation. A series of new compounds were prepared conveniently and characterized by IR, 1 H NMR, MS, and elemental analysis. The preliminary bioassays results revealed that they have certain antimicrobial activity against Bacillus subtilis, Staphylococcus aureus, and Aspergillus fumigatus.

4‐Quinolone Derivatives and Their Activities Against Gram‐negative Pathogens

“…A variety of 4‐quinolones with N‐1 position bearing unsaturated alkyl , amino , sulfonyl , ester , carboxylic acids , imidazole , 1,2,4‐triazole , heterocycles , and N‐1/C‐8 1,2,4‐oxadiazine and N‐1/C‐8 imidazole as well as N‐1 ethylene tethered quinolone dimers were screened for their in vitro antibacterial activities against a panel of clinically relevant Gram‐negative pathogens. In spite of a significant part of them were less potent than the references, the enriched SAR paved the way to the further rational optimization of 4‐quinolones.…”