BMS-247243

Methicillin-resistant Staphylococcus aureus (MRSA) is now one of the commonest causes of nosocomial infection worldwide. The mainstay of treatment until now has been the glycopeptides (vancomycin and teicoplanin). They are not without toxicity and need parenteral administration and monitoring of levels. The increasing frequency of MRSA infections, coupled with the emergence of glycopeptide resistance in S. aureus has made the introduction of new drugs active against Gram-positive organisms essential. New agents active against Gram-positive organisms represent either genuinely novel classes of antimicrobials (e.g., oxazolidinones and lipoproteins) or those derived from existing classes (e.g., tetracyclines, glycopeptides, streptogramins and cephalosporins). Some of these newer antibiotics appear to be effective against multi-resistant organisms including MRSA.

BMS-247243, a novel cephalosporin inhibitory for methicillin-resistant staphylococci, primarily has activity against gram-positive bacteria. The activities of BMS-247243, cefotaxime, and ceftriaxone against streptococci and Streptococcus pneumoniae were similar. BMS-247243 inhibits Enterococcus faecalis but not Enterococcus faecium . BMS-247243 also inhibits many inherently vancomycin-resistant species ( Leuconstoc , Lactobacillus , Pediococcus ) and anaerobic gram-positive bacteria.