Structure-based design of beta-lactamase inhibitors. 2. Synthesis and evaluation of bridged sulfactams and oxamazins |
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| Authors: | C Hubschwerlen P Angehrn K Gubernator MG Page JL Specklin |
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| Affiliation: | Preclinical Research, F. Hoffmann-La Roche Ltd., CH-4070 Basle, Switzerland. |
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| 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. |
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