Novel quinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV.

Mitton-Fry, Mark J; Brickner, Steven J; Hamel, Judith C; Brennan, Lori; Casavant, Jeffrey M; Chen, Michael; Chen, Tao; Ding, Xiaoyuan; Driscoll, James; Hardink, Joel; Hoang, Thuy; Hua, Erbing; Huband, Michael D; Maloney, Meghan; Marfat, Anthony; McCurdy, Sandra P; McLeod, Dale; Plotkin, Michael; Reilly, Usa; Robinson, Shaughn; Schafer, John; Shepard, Richard M; Smith, James F; Stone, Gregory G; Subramanyam, Chakrapani; Yoon, Kwansik; Yuan, Wei; Zaniewski, Richard P; Zook, Christopher

Mitton-Fry, Mark J; Brickner, Steven J; Hamel, Judith C; Brennan, Lori; Casavant, Jeffrey M; Chen, Michael; Chen, Tao; Ding, Xiaoyuan; Driscoll, James; Hardink, Joel; Hoang, Thuy; Hua, Erbing; Huband, Michael D; Maloney, Meghan; Marfat, Anthony; McCurdy, Sandra P; McLeod, Dale; Plotkin, Michael; Reilly, Usa; Robinson, Shaughn; Schafer, John; Shepard, Richard M; Smith, James F; Stone, Gregory G; Subramanyam, Chakrapani; Yoon, Kwansik; Yuan, Wei; Zaniewski, Richard P; Zook, Christopher.

Affiliation

Mitton-Fry MJ; Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA. mjmitton@owu.edu

Bioorg Med Chem Lett ; 23(10): 2955-61, 2013 May 15.

Article in En | MEDLINE | ID: mdl-23566517

ABSTRACT

ABSTRACT

A structurally novel set of inhibitors of bacterial type II topoisomerases with potent in vitro and in vivo antibacterial activity was developed. Dual-targeting ability, hERG inhibition, and pharmacokinetic properties were also assessed.

Subject(s)

Anti-Bacterial Agents/pharmacology; DNA Topoisomerase IV/antagonists & inhibitors; Enzyme Inhibitors/pharmacology; Quinolines/pharmacology; Staphylococcus aureus/drug effects; Streptococcus pneumoniae/drug effects; Topoisomerase II Inhibitors; Animals; Anti-Bacterial Agents/administration & dosage; Anti-Bacterial Agents/chemistry; DNA Gyrase/metabolism; DNA Topoisomerase IV/metabolism; DNA Topoisomerases, Type II/metabolism; Dose-Response Relationship, Drug; Enzyme Inhibitors/administration & dosage; Enzyme Inhibitors/chemistry; Ether-A-Go-Go Potassium Channels/antagonists & inhibitors; Humans; Microbial Sensitivity Tests; Molecular Structure; Quinolines/administration & dosage; Quinolines/chemistry; Rats; Staphylococcus aureus/enzymology; Streptococcus pneumoniae/enzymology; Structure-Activity Relationship

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinolines / Staphylococcus aureus / Streptococcus pneumoniae / DNA Topoisomerase IV / Enzyme Inhibitors / Topoisomerase II Inhibitors / Anti-Bacterial Agents Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2013 Document type: Article Affiliation country: United States Publication country: ENGLAND / ESCOCIA / GB / GREAT BRITAIN / INGLATERRA / REINO UNIDO / SCOTLAND / UK / UNITED KINGDOM

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