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通过嵌段合成方法制备抗菌β-类肽。

Antimicrobial beta-peptoids by a block synthesis approach.

作者信息

Shuey Steven W, Delaney William J, Shah Mukesh C, Scialdone Mark A

机构信息

DuPont Central Research and Development, PO Box 80328, Experimental Station, Wilmington, DE 19880-0328, USA.

出版信息

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1245-8. doi: 10.1016/j.bmcl.2005.11.075. Epub 2005 Dec 27.

DOI:10.1016/j.bmcl.2005.11.075
PMID:16384703
Abstract

Antimicrobial peptides and their mimetics offer a potential new disinfective tool. beta-Peptoids (oligo-N-substituted beta-alanines) were synthesized and investigated for antimicrobial activity. A block approach whereby di- and tri-beta-peptoids were first prepared and then ligated via amide bond formation to synthesize larger beta-peptoids was developed. The beta-peptoids were found to possess moderate activity in an Escheridchia coli assay.

摘要

抗菌肽及其模拟物提供了一种潜在的新型消毒工具。合成了β-类肽(寡聚N-取代β-丙氨酸)并研究其抗菌活性。开发了一种分段方法,先制备二聚体和三聚体β-类肽,然后通过酰胺键形成进行连接以合成更大的β-类肽。结果发现β-类肽在大肠杆菌检测中具有中等活性。

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