National Center for
3S1Y: Amp-c Beta-lactamase (pseudomonas Aeruginosa) In Complex With A Beta- Lactamase Inhibitor
Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712
Bioorg. Med. Chem. Lett. (2011) 21 p.4267-4270
The bridged monobactam beta-lactamase inhibitor MK-8712 (1) effectively inhibits class C beta-lactamases. Side chain N-alkylated and ring-opened analogs of 1 were prepared and evaluated for combination with imipenem to overcome class C beta-lactamase mediated resistance. Although some analogs were more potent inhibitors of AmpC, none exhibited better synergy with imipenem than 1.