Synthesis and biological testing of non-Fluorinated analogues of levofloxacin

Quinolones without the usual 6-fluorine substituent have been recently described as potent antibacterial agents. A series of non-fluorinated analogues of the antibacterial quinolone Levofloxacin were synthesized and tested. The synthesis of a series of novel quinolone antibacterials including the no...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-07, Vol.13 (14), p.2373-2375
Hauptverfasser:	Gray, Jeffrey L., Almstead, Ji-In K., Gallagher, Corey P., Hu, X.Eric, Kim, Nick K., Taylor, Cynthia J., Twinem, Tracy L., Wallace, Cynthia D., Ledoussal, Benoit
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Infective Agents - chemical synthesis Anti-Infective Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Bacteria - drug effects Biological and medical sciences Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Escherichia coli - drug effects Levofloxacin Medical sciences Microbial Sensitivity Tests Molecular Conformation Ofloxacin - analogs & derivatives Ofloxacin - chemical synthesis Ofloxacin - pharmacology Pharmacology. Drug treatments Structure-Activity Relationship Topoisomerase II Inhibitors
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Beschreibung
Zusammenfassung:	Quinolones without the usual 6-fluorine substituent have been recently described as potent antibacterial agents. A series of non-fluorinated analogues of the antibacterial quinolone Levofloxacin were synthesized and tested. The synthesis of a series of novel quinolone antibacterials including the non-fluorinated analogue of Levofloxacin ( 1) is reported.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00399-8