Anti-MRSA cephems. Part 3: Additional C-7 acid derivatives

Twenty-seven novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds contain novel acid moieties at C-7 that were synthesized using nucleophilic aromatic substitution reactions and Stille couplings. The most interesting compound ( 6) displayed an MIC 90 against MRSA of 3.7 μg/mL, and an average PD 50 of 3.9 mg/kg. Novel C-7 acid cephalosporin derivatives with good activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The most interesting compound ( 6) displayed an MIC 90 against MRSA of 3.7 μg/mL, and an average PD 50 of 3.9 mg/kg..