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

被引：4

作者：

Crauste, Celine ^{[1
]}

Froeyen, Matheus ^{[1
]}

Anne, Jozef ^{[2
]}

Herdewijn, Piet ^{[1
]}

机构：

[1] Katholieke Univ Leuven, Rega Inst Med Res, Med Chem Lab, B-3000 Louvain, Belgium

[2] Katholieke Univ Leuven, Rega Inst Med Res, Dept Microbiol & Immunol, B-3000 Louvain, Belgium

来源：

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY | 2011年 / 2011卷 / 19期

关键词：

Medicinal chemistry; Antibiotics; Enzymes; Peptides; Lactams; Asymmetric synthesis; ENANTIOSELECTIVE SYNTHESIS; BIOLOGICAL EVALUATION; PENEM INHIBITORS; SERINE PROTEASES; MITSUNOBU; ANTIBIOTICS; DESIGN; ELASTASE; CYSTEINE; ENZYME;

D O I：

10.1002/ejoc.201100148

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

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.

引用

页码：3437 / 3449

页数：13

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