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Anti-MRSA cephems. Part 1: C-3 substituted thiopyridinium derivatives
D M Springer1, B Y Luh, J J Bronson
1Anti-infective Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA. springed@bms.com
Bioorganic & Medicinal Chemistry Letters
|March 30, 2001
Abstract:
Sixteen novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds were synthesized using substituted thiopyridones, generated either by cyclization of functionalized precursors, or by direct alkylation of the enolate of 2-methyl substituted pyrones. The most active compound in vitro against a strain of MRSA (A27223) displayed an MIC of 0.5 microg/mL. The most efficacious compound in vivo had a PD50 of 2.1 mg/kg.