Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced pK(a): antibacterial agents with an improved safety profile.

Reck, Folkert; Alm, Richard A; Brassil, Patrick; Newman, Joseph V; Ciaccio, Paul; McNulty, John; Barthlow, Herbert; Goteti, Kosalaram; Breen, John; Comita-Prevoir, Janelle; Cronin, Mark; Ehmann, David E; Geng, Bolin; Godfrey, Andrew Aydon; Fisher, Stewart L

Reck, Folkert; Alm, Richard A; Brassil, Patrick; Newman, Joseph V; Ciaccio, Paul; McNulty, John; Barthlow, Herbert; Goteti, Kosalaram; Breen, John; Comita-Prevoir, Janelle; Cronin, Mark; Ehmann, David E; Geng, Bolin; Godfrey, Andrew Aydon; Fisher, Stewart L.

Affiliation

Reck F; Infection Innovative Medicines Unit, AstraZeneca R&D Boston , 35 Gatehouse Drive, Waltham, Massachusetts 02451, United States. folkert.reck@novartis.com

J Med Chem ; 55(15): 6916-33, 2012 Aug 09.

Article in En | MEDLINE | ID: mdl-22779424

Subject(s)

Anti-Bacterial Agents/chemical synthesis; Dioxanes/chemical synthesis; Piperidines/chemical synthesis; Quinolones/chemical synthesis; Topoisomerase II Inhibitors/chemical synthesis; Administration, Oral; Animals; Anti-Bacterial Agents/pharmacology; Anti-Bacterial Agents/toxicity; Biological Availability; DNA Topoisomerase IV/antagonists & inhibitors; Dioxanes/pharmacology; Dioxanes/toxicity; Dogs; Drug Resistance, Bacterial; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels/antagonists & inhibitors; Guinea Pigs; Methicillin-Resistant Staphylococcus aureus; Mice; Microbial Sensitivity Tests; Piperidines/pharmacology; Piperidines/toxicity; Quinolones/pharmacology; Quinolones/toxicity; Staphylococcal Infections/drug therapy; Staphylococcal Infections/microbiology; Stereoisomerism; Structure-Activity Relationship; Topoisomerase II Inhibitors/pharmacology; Topoisomerase II Inhibitors/toxicity

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Quinolones / Dioxanes / Topoisomerase II Inhibitors / Anti-Bacterial Agents Type of study: Prognostic_studies Limits: Animals Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2012 Type: Article Affiliation country: United States

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