The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not possess a &bgr;-lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as &bgr;-lactamase inhibitors and as antibiotics.
本发明提供了新型&bgr;-内酰胺酶
抑制剂,这些
抑制剂在结构上与目前可用的
天然产物和半合成&bgr;-内酰胺酶
抑制剂无关,并且不具有&bgr;-内酰胺药理源。这些新型
抑制剂是完全合成的,可以随时获得各种结构相关的类似物。这些新
抑制剂的某些实施方案还能与细菌的 DD 肽酶结合,因此有可能既作为&bgr;-内酰胺酶
抑制剂,又作为抗生素。