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

作者：Crauste Celine; Froeyen Matheus; Anne Jozef; Herdewijn Piet^*

来源：European Journal of Organic Chemistry, 2011, 2011(19): 3437-3449.

DOI：10.1002/ejoc.201100148

• Medicinal chemistry
• Antibiotics
• Enzymes
• Peptides
• Lactams
• Asymmetric synthesis

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.

• 出版日期2011-7
• 单位河北医科大学