基于结构的β-内酰胺酶抑制剂设计。2. 桥连硫代内酰胺和恶唑嗪的合成与评价。
Structure-based design of beta-lactamase inhibitors. 2. Synthesis and evaluation of bridged sulfactams and oxamazins.
作者信息
Hubschwerlen C, Angehrn P, Gubernator K, Page M G, Specklin J L
机构信息
Preclinical Research, F. Hoffmann-La Roche Ltd., CH-4070 Basle, Switzerland.
出版信息
J Med Chem. 1998 Oct 8;41(21):3972-5. doi: 10.1021/jm9800245.
PMID:9767634
Abstract
A series of bridged monocyclic beta-lactams activated by various groups on the beta-lactam nitrogen (X = OCH2CO2H, OSO3H) has been synthesized and evaluated. Among them, the bridged sulfactams (X = OSO3H) were found to be effective beta-lactamase inhibitors. They inhibit both class A and class C beta-lactamases.
摘要
已经合成并评估了一系列在β-内酰胺氮上由各种基团活化的桥连单环β-内酰胺（X = OCH2CO2H，OSO3H）。其中，桥连磺胺类（X = OSO3H）被发现是有效的β-内酰胺酶抑制剂。它们抑制A类和C类β-内酰胺酶。
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