Design, synthesis, and structure-activity relationship studies of ATP analogues as DNA gyrase inhibitors.
We report herein the design and synthesis of ATP-analogues, namely 4-amino-pyrazolo[3,4-d]pyrimidines and 4-amino-pyrazolo[1,5-a][1,3,5]triazines, with DNA gyrase inhibitory activity. Among these series, some compounds exhibited promising antibacterial activity.
Lübbers
T
T
Department of Infectious Diseases, F. Hoffmann-La Roche Ltd., Basel, Switzerland. thomas.luebbers@roche.com
Angehrn
P
P
Gmünder
H
H
Herzig
S
S
Kulhanek
J
J
D000255:Adenosine Triphosphate / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000201:enzymology; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D059005:Topoisomerase II Inhibitors; D000255:Adenosine Triphosphate