Abstract
Forty-five novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds contain novel cinnamic acid moieties at C-7 that were synthesized using a key Heck reaction followed by nucleophilic aromatic substitution reactions. The most active compound ( 41) displayed an MIC 90 against MRSA of 1.0 μg/mL, and a PD 50 of 0.8 mg/kg. Compound 14 was found to be very safe in a mouse model of acute toxicity.
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