Synthesis and structural-activity relationships of 3-hydroxyquinazoline-2,4-dione antibacterial agents.
A series of 3-hydroxyquinazoline-2,4-diones was synthesized and evaluated for antibacterial activity. This series represents a novel addition to the DNA gyrase inhibitor class of antibacterials. Appropriate substitutions onto the core template yielded compounds with excellent potency against E. coli gyrase and significant in vitro Gram-negative and Gram-positive antibacterial activity.
Tran
Tuan P
TP
Department of Chemistry, Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Road, MI 48105, USA. tuan.tran@pfizer.com
Ellsworth
Edmund L
EL
Stier
Michael A
MA
Domagala
John M
JM
Showalter
H D
HD
Gracheck
Stephen J
SJ
Shapiro
Martin A
MA
Joannides
Themis E
TE
Singh
Rajeshwar
R
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis*; D006912:Hydroxyquinolines / Q000138:chemical synthesis; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D011799:Quinazolines / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D006912:Hydroxyquinolines; D011799:Quinazolines