Abstract
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 microg/mL, and an average PD(50) of 3.9 mg/kg.
MeSH terms
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Animals
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / pharmacology*
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Cephalosporins / chemistry*
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Cephalosporins / pharmacology*
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Disease Models, Animal
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Lethal Dose 50
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Methicillin Resistance
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Mice
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Microbial Sensitivity Tests
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Staphylococcal Infections / microbiology
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Staphylococcus aureus / drug effects*
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Staphylococcus aureus / pathogenicity
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Cephalosporins