Side chain SAR of bicyclic ß-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712.

ABSTRACT

The bridged monobactam ß-lactamase inhibitor MK-8712 (1) effectively inhibits class C ß-lactamases. Side chain N-alkylated and ring-opened analogs of 1 were prepared and evaluated for combination with imipenem to overcome class C ß-lactamase mediated resistance. Although some analogs were more potent inhibitors of AmpC, none exhibited better synergy with imipenem than 1.