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DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: synthesis and antibacterial activity.
East, Stephen P; White, Clara Bantry; Barker, Oliver; Barker, Stephanie; Bennett, James; Brown, David; Boyd, E Andrew; Brennan, Christopher; Chowdhury, Chandana; Collins, Ian; Convers-Reignier, Emmanuelle; Dymock, Brian W; Fletcher, Rowena; Haydon, David J; Gardiner, Mihaly; Hatcher, Stuart; Ingram, Peter; Lancett, Paul; Mortenson, Paul; Papadopoulos, Konstantinos; Smee, Carol; Thomaides-Brears, Helena B; Tye, Heather; Workman, James; Czaplewski, Lloyd G.
Bioorg Med Chem Lett ; 19(3): 894-9, 2009 Feb 01.
Article in English | MEDLINE | ID: mdl-19095445

ABSTRACT

The synthesis and antibacterial activities of three chemotypes of DNA supercoiling inhibitors based on imidazolo[1,2-a]pyridine and [1,2,4]triazolo[1,5-a]pyridine scaffolds that target the ATPase subunits of DNA gyrase and topoisomerase IV (GyrB/ParE) is reported. The most potent scaffold was selected for optimization leading to a series with potent Gram-positive antibacterial activity and a low resistance frequency.


Subject(s)
Anti-Infective Agents/pharmacology , Chemistry, Pharmaceutical/methods , DNA Topoisomerase IV/antagonists & inhibitors , Topoisomerase II Inhibitors , Adenosine Triphosphatases/antagonists & inhibitors , Adenosine Triphosphatases/chemistry , Drug Design , Enterococcus faecalis/metabolism , Escherichia coli/metabolism , Gram-Positive Bacteria/metabolism , Humans , Imidazoles/chemistry , Inhibitory Concentration 50 , Pyridines/chemistry , Staphylococcus aureus/metabolism , Structure-Activity Relationship , Triazoles/chemistry
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