Pyridoquinoxaline N-oxides. 2. Synthesis and antibacterial activity of tricyclic lactams.
A series of novel 3,4-dihydropyrido[3,4-b]quinoxalin-1(2H)-one 5,10-dioxides was synthesized using an intramolecular amidation reaction. The lactams were screened in vitro and in vivo against Salmonella choleraesuis, Pasteurella multocida, and Escherichia coli. An N-methyl analogue was the most potent member of this series, with antibacterial activity comparable to that of the commercially important quinoxaline 1,4-dioxide carbadox.
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis*; D001419:Bacteria / Q000187:drug effects; D001424:Bacterial Infections / Q000188:drug therapy; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D007769:Lactams / Q000138:chemical synthesis / Q000494:pharmacology; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology; D012475:Salmonella / Q000187:drug effects
D000900:Anti-Bacterial Agents; D007769:Lactams; D011810:Quinoxalines