Asymmetric Synthesis of New beta-Lactam Lipopeptides as Bacterial Signal Peptidase I Inhibitors

[摘要]：The transmembrane bacterial enzyme, signal peptidase I, is recognized as being a promising target for reducing the emergence of drug resistance. The asymmetric synthesis and the biological evaluation of original beta-lactam lipopeptides have been performed to discover potent signal peptidase inhibitors. The importance of the azetidinone motif of these lipopeptides has been demonstrated and can serve as a starting point to exploit and improve the reactivity of the beta-lactam in peptidomimetics.

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