A library of substituted 6-pyridylmethylidenepenicillin sulfones was prepared and evaluated as inhibitors of representative class A, C, and D �-lactamases, including class A and D carbapenemases, and also for synergy with imipenem against resistant strains of Pseudomonas aeruginosa, Klebsiella pneumoniae, and Acinetobacter baumannii.  The compounds were potent inhibitors of the representative serine �-lactamases, and, with appropriate substitution patterns, could display synergy with imipenem against resistant Gram-negative pathogens.  The synthesis, as well as the biochemical and microbiological activity will be presented, together with a synopsis of the SAR trends.

Understanding SARs of the 6-alkylidenepenicillin sulfones, potent inhibitors of Class A, C, and D �-lactamases

247th National Meeting (2014)

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