Synthesis and biological evaluation of benzo[b]naphthyridones, a series of new topical antibacterial agents.
We describe here the synthesis and biological evaluation of a series of benzo[b]naphthyridones, a new family of tricyclic antibacterial compounds that have a gram-positive spectrum of activity. RP60556A, one of the most potent of these compounds, is bactericidal against multiresistant cocci, especially multiresistant Staphylococcus aureus strains. Its physico-chemical and biological properties make it particularly suitable for topical antibacterial use.
Tabart
M
M
Agents Pharma, Centre de Recherche de Vitry Alfortville, Vitry sur Seine, France. michel.tabart@aventis.com
Picaut
G
G
Desconclois
J F
JF
Dutka-Malen
S
S
Huet
Y
Y
Berthaud
N
N
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000891:Anti-Infective Agents, Local / Q000138:chemical synthesis / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D018432:Drug Resistance, Multiple; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D006168:Guinea Pigs; D008826:Microbial Sensitivity Tests; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013207:Staphylococcal Skin Infections / Q000188:drug therapy; D013211:Staphylococcus aureus / Q000187:drug effects*
D000900:Anti-Bacterial Agents; D000891:Anti-Infective Agents, Local; D009287:Naphthyridines; D010879:Piperazines; C433951:RP60556A