Monocyclic and tricyclic analogs of quinolones: mechanism of action.
The mode of action of Ro 13-5478 and Ro 14-9578, monocyclic and tricyclic quinolone analogs, respectively, was examined for Escherichia coli and Staphylococcus aureus. The compounds showed antibacterial activity and effects on cell morphology, replicative DNA biosynthesis, and gyrase-catalyzed DNA supercoiling that were comparable to those shown by nalidixic acid and by oxolinic acid compounds. The results suggest that their site of action is DNA gyrase and that a bicyclic quinolone nucleus is not essential for activity.
D042462:4-Quinolones; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D000890:Anti-Infective Agents; D004261:DNA Replication / Q000187:drug effects; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D004269:DNA, Bacterial / Q000378:metabolism; D004278:DNA, Superhelical / Q000378:metabolism; D004926:Escherichia coli / Q000187:drug effects*; D007711:Klebsiella pneumoniae / Q000187:drug effects; D009268:Nalidixic Acid / Q000494:pharmacology; D009539:Nicotinic Acids / Q000494:pharmacology; D010093:Oxolinic Acid / Q000494:pharmacology; D011804:Quinolines / Q000494:pharmacology*; D015363:Quinolones; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship
D042462:4-Quinolones; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D004269:DNA, Bacterial; D004278:DNA, Superhelical; D009539:Nicotinic Acids; D011804:Quinolines; D015363:Quinolones; C052872:Ro 14-9578; D009268:Nalidixic Acid; C052871:Ro 13-5478; D004250:DNA Topoisomerases, Type II; D010093:Oxolinic Acid