3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
The 3-aminoquinzolinediones represent a new series of antibacterial agents structurally related to the fluoroquinolones. They are inhibitors of bacterial gyrase and topoisomerase IV and demonstrate clinically useful antibacterial activity against fastidious Gram-negative and Gram-positive organisms, including multidrug- and fluoroquinolone-resistant organisms. These agents also demonstrate in vivo efficacy in murine systemic infection models.
Ellsworth
Edmund L
EL
Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. edmund.ellsworth@pfizer.com
Tran
Tuan P
TP
Showalter
H D Hollis
HD
Sanchez
Joseph P
JP
Watson
Brian M
BM
Stier
Michael A
MA
Domagala
John M
JM
Gracheck
Stephen J
SJ
Joannides
E Themis
ET
Shapiro
Martin A
MA
Dunham
Steve A
SA
Hanna
Debra L
DL
Huband
Michael D
MD
Gage
Jeffrey W
JW
Bronstein
Joel C
JC
Liu
Jia Yeu
JY
Nguyen
Dai Q
DQ
Singh
Rajeshwar
R
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D027101:DNA Topoisomerase IV / Q000037:antagonists & inhibitors; D024901:Drug Resistance, Multiple, Bacterial / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D052999:Quinazolinones / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D052999:Quinazolinones; D059005:Topoisomerase II Inhibitors; D027101:DNA Topoisomerase IV