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将杂环并入缩肽骨架中,以生成多种缩肽类启发的一珠一化合物库。

Incorporation of heterocycles into the backbone of peptoids to generate diverse peptoid-inspired one bead one compound libraries.

机构信息

Department of Chemistry, The Scripps Research Institute, Scripps Florida , Jupiter, Florida 33458, United States.

出版信息

ACS Comb Sci. 2012 Mar 12;14(3):164-9. doi: 10.1021/co200195t. Epub 2012 Feb 21.

Abstract

Combinatorial libraries of peptoids (oligo-N-substituted glycines) have proven to be useful sources of protein ligands. Each unit of the peptoid oligomer is derived from 2-haloacetic acid and a primary amine. To increase the chemical diversity available in peptoid libraries, we demonstrate here that heterocyclic halomethyl carboxylic acids can be employed as backbone building blocks in the synthesis of peptoid-based oligomers. Optimized conditions are reported that allow the creation of large, high quality combinatorial libraries containing these units.

摘要

肽核酸(寡 N-取代甘氨酸)的组合文库已被证明是蛋白质配体的有用来源。肽核酸寡聚物的每个单元都来自 2-卤代乙酸和伯胺。为了增加肽核酸文库中的化学多样性,我们在此证明杂环卤代甲基羧酸可用作合成基于肽核酸的寡聚物的骨架构建块。报道了优化的条件,允许创建包含这些单元的大型、高质量的组合文库。

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