Anti-MRSA cephems. Part 2: C-7 cinnamic acid derivatives

DM Springer, BY Luh, J Goodrich, JJ Bronson

Index: Springer, Dane M.; Luh, Bing-Yu; Goodrich, Jason; Bronson, Joanne J. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 2 p. 265 - 279

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Citation Number: 22

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 MIC90 against MRSA of 1.0 μg/mL, and a PD50 of 0.8 mg/kg. Compound 14 was found to be very safe in ...

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