1.
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
2.
Bioorg Med Chem Lett
; 19(2): 524-7, 2009 Jan 15.
Article
in English
| MEDLINE
| ID: mdl-19064318
ABSTRACT
3-Methoxybenzamide is a weak inhibitor of the essential bacterial cell division protein FtsZ. Exploration of the structure-activity relationships of 3-methoxybenzamide analogues led to the identification of potent anti-staphylococcal compounds.