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Bioorg Med Chem Lett ; 21(24): 7489-95, 2011 Dec 15.
Article in English | MEDLINE | ID: mdl-22047689

ABSTRACT

We have identified a series of amino-piperidine antibacterials with a good broad spectrum potency. We report the investigation of various subunits in this series and advanced studies on compound 8. Compound 8 possesses good pharmacokinetics, broad spectrum antibacterial activity and demonstrates oral efficacy in a rat lung infection model.


Subject(s)
Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , DNA Topoisomerases, Type II/chemistry , Dioxanes/chemistry , Dioxanes/pharmacology , Naphthyridines/chemistry , Naphthyridines/pharmacology , Piperidines/chemistry , Topoisomerase II Inhibitors/chemistry , Animals , Anti-Bacterial Agents/therapeutic use , DNA Topoisomerases, Type II/metabolism , Dioxanes/therapeutic use , Disease Models, Animal , Dogs , Haplorhini , Humans , Lung Diseases/drug therapy , Microbial Sensitivity Tests , Naphthyridines/therapeutic use , Piperidines/pharmacology , Piperidines/therapeutic use , Rats , Structure-Activity Relationship , Topoisomerase II Inhibitors/pharmacology , Topoisomerase II Inhibitors/therapeutic use
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