Structure-activity relationship in two series of aminoalkyl substituted coumarin inhibitors of gyrase B.
Two series of aminosubstituted coumarins were synthesised and evaluated in vitro as inhibitors of DNA gyrase and as potential antibacterials. Novel novobiocin-like coumarins, 4-(dialkylamino)methylcoumarins and 4-((2-alkylamino)ethoxy)coumarins, were discovered as gyrase B inhibitors with promising antibacterial activity in vitro.
Laurin
P
P
Medicinal Chemistry, Hoechst Marion Roussel, Romainville, France.
Ferroud
D
D
Schio
L
L
Klich
M
M
Dupuis-Hamelin
C
C
Mauvais
P
P
Lassaigne
P
P
Bonnefoy
A
A
Musicki
B
B
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology; D027081:DNA Gyrase; D004278:DNA, Superhelical / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D004926:Escherichia coli / Q000201:enzymology; D006094:Gram-Positive Bacteria / Q000187:drug effects; D015394:Molecular Structure; D009675:Novobiocin / Q000031:analogs & derivatives / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000494:pharmacology; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
D000900:Anti-Bacterial Agents; D003374:Coumarins; D004278:DNA, Superhelical; D004791:Enzyme Inhibitors; D010456:Peptides, Cyclic; D059005:Topoisomerase II Inhibitors; C085889:cyclothialidine; D009675:Novobiocin; C006260:clorobiocin; D027081:DNA Gyrase