title: Structure-activity relationship in two series of aminoalkyl substituted coumarin inhibitors of gyrase B.
abstract: 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.
authors.affiliation: Medicinal Chemistry, Hoechst Marion Roussel, Romainville, France.
authors.forename: P
authors.initials: P
authors.lastname: Laurin
authors.forename: D
authors.initials: D
authors.lastname: Ferroud
authors.forename: L
authors.initials: L
authors.lastname: Schio
authors.forename: M
authors.initials: M
authors.lastname: Klich
authors.forename: C
authors.initials: C
authors.lastname: Dupuis-Hamelin
authors.forename: P
authors.initials: P
authors.lastname: Mauvais
authors.forename: P
authors.initials: P
authors.lastname: Lassaigne
authors.forename: A
authors.initials: A
authors.lastname: Bonnefoy
authors.forename: B
authors.initials: B
authors.lastname: Musicki
mesh_terms: 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
chemical_list: 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