| Structural highlights
Publication Abstract from PubMed
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.
Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712.,Chen H, Blizzard TA, Kim S, Wu J, Young K, Park YW, Ogawa AM, Raghoobar S, Painter RE, Wisniewski D, Hairston N, Fitzgerald P, Sharma N, Scapin G, Lu J, Hermes J, Hammond ML Bioorg Med Chem Lett. 2011 Jul 15;21(14):4267-70. doi:, 10.1016/j.bmcl.2011.05.065. Epub 2011 May 27. PMID:21676616[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
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References
- ↑ Chen H, Blizzard TA, Kim S, Wu J, Young K, Park YW, Ogawa AM, Raghoobar S, Painter RE, Wisniewski D, Hairston N, Fitzgerald P, Sharma N, Scapin G, Lu J, Hermes J, Hammond ML. Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4267-70. doi:, 10.1016/j.bmcl.2011.05.065. Epub 2011 May 27. PMID:21676616 doi:10.1016/j.bmcl.2011.05.065
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