Download MendeleySide chain SAR of bicyclic Beta-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712
Chen, H., Blizzard, T.A., Kim, S., Wu, J., Young, K., Park, Y.W., Ogawa, A.M., Raghoobar, S., Painter, R.E., Wisniewski, D., Hairston, N., Fitzgerald, P., Sharma, N., Scapin, G., Lu, J., Hermes, J., Hammond, M.L.(2011) Bioorg Med Chem Lett 21: 4267-4270
- PubMed: 21676616
- DOI: https://doi.org/10.1016/j.bmcl.2011.05.065
- Primary Citation of Related Structures:
3S1Y, 3S22 - PubMed Abstract:
The bridged monobactam β-lactamase inhibitor MK-8712 (1) effectively inhibits class C β-lactamases. Side chain N-alkylated and ring-opened analogs of 1 were prepared and evaluated for combination with imipenem to overcome class C β-lactamase mediated resistance. Although some analogs were more potent inhibitors of AmpC, none exhibited better synergy with imipenem than 1.
Organizational Affiliation:
Departments of Medicinal Chemistry, Merck Research Labs, Rahway, NJ 07065, USA. helen_chen@merck.com
