Antimicrobial activity against Staphylococcus aureus of semisynthetic injectable streptogramins: RP 59500 and related compounds.
Pristinamycin displays unique antibacterial properties due to the synergy between its two components, pristinamycin I and pristinamycin II. Because this antibiotic is not water-soluble, its administration is restricted to the oral route, and its therapeutic potential is thereby limited. Novel water-soluble derivatives of the naturally-occurring antibiotic pristinamycin were obtained by modifications of its two major components. The modifications included regioselective and stereoselective substitution alpha to the carbonyl group in the 4-oxo-pipecolic acid residue of pristinamycin IA (PIA) and stereoselective conjugate addition to the double bond of the dehydroproline ring in pristinamycin IIA (PIIA). We report here the in-vitro and in-vivo activities of some representative water-soluble derivatives of pristinamycin IA and pristinamycin IIA against Staphylococcus aureus reference strains, sensitive or resistant to methicillin and/or macrolides.
Barrière
J C
JC
Rhone-Poulenc Rorer, Centre de Recherche de Vitry-Alfortville, Vitry sur Seine, France.
Bouanchaud
D H
DH
Paris
J M
JM
Rolin
O
O
Harris
N V
NV
Smith
C
C
D000818:Animals; D004338:Drug Combinations; D051379:Mice; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects*; D014769:Virginiamycin / Q000031:analogs & derivatives / Q000494:pharmacology*
D004338:Drug Combinations; D014769:Virginiamycin; C062940:quinupristin-dalfopristin