Synthesis and antimicrobial activity of DNA-gyrase inhibiting derivatives of 4-oxo-1,4-dihydro-3-pyridinecarboxylic acid.
A series of 6-substituted-1-aryl-4-oxo-1,4-dihydronicotinic acids were synthesised as monocyclic analogues of the quinolones. The 6-(2-aryl-1-methylethenyl)- and of the 6-(2-arylethenyl)-substituted compounds were shown to possess antibacterial properties that correlate with DNA gyrase inhibitory activity. Differently from the quinolones the antimicrobial activity of the compounds of this study is predominantly against Gram positive strains. The structure-activity relationships ascertained for these monocyclic compounds differ from those established for the quinolones.
Department of Chemistry, Glaxo S.p.a. Research Laboratories, Verona, Italy.
C
C
Bassini
C
C
Bismara
R
R
Carlesso
A
A
Feriani
G
G
Gaviraghi
C
C
Marchioro
A
A
Perboni
R E
RE
Shaw
B
B
Tamburini
G
G
Tarzia
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D009539:Nicotinic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
D000900:Anti-Bacterial Agents; D009539:Nicotinic Acids; D059005:Topoisomerase II Inhibitors