双环β-内酰胺酶抑制剂 (BLIs) 的侧链 SAR。2. MK-8712 的 N-烷基化和开链类似物。
Side chain SAR of bicyclic β-lactamase inhibitors (BLIs). 2. N-Alkylated and open chain analogs of MK-8712.
机构信息
Departments of Medicinal Chemistry, Merck Research Labs, Rahway, NJ 07065, USA.
出版信息
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
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.
摘要
桥连单环β-内酰胺酶抑制剂 MK-8712（1）能有效抑制 C 类β-内酰胺酶。制备并评价了 1 的侧链 N-烷基化和环开环类似物，以与亚胺培南联合使用来克服 C 类β-内酰胺酶介导的耐药性。尽管一些类似物对 AmpC 的抑制作用更强，但没有一种比 1 与亚胺培南的协同作用更好。
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