M. Ishiguro et al., 5,6-CIS-PENEMS - BROAD-SPECTRUM ANTI-METHICILLIN-RESISTANT STAPHYLOCOCCUS-AUREUS BETA-LACTAM ANTIBIOTICS, Journal of medicinal chemistry, 40(14), 1997, pp. 2126-2132
5,6-cis-Penem derivatives have been synthesized and evaluated as anti-
MRSA antibiotics. The cis-penems 5 and 6 showed potent activities agai
nst not only MRSA but also a wide variety of bacteria including beta-l
actamase-producing microorganisms. These compounds were designed to ha
ve high affinity to the penicillin-binding protein 2a of MRSA and to f
orm stable acyl intermediates with beta-lactamases by blocking the dea
cylating water molecule.