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高度官能化的环状β-氨基酸部分作为肽研究和药物设计中有前途的支架。

Highly functionalized cyclic β-amino acid moieties as promising scaffolds in peptide research and drug design.

机构信息

Institute of Pharmaceutical Chemistry, University of Szeged, Eötvös u. 6, 6720, Szeged, Hungary.

MTA-SZTE Stereochemistry Research Group, Hungarian Academy of Sciences, Eötvös u. 6, 6720, Szeged, Hungary.

出版信息

Amino Acids. 2017 Sep;49(9):1441-1455. doi: 10.1007/s00726-017-2439-9. Epub 2017 May 30.

Abstract

Peptide-based drug research has received high attention in the field of medicinal chemistry over the past decade. For drug design, to improve proteolytic stability, it is desirable to include unnatural building blocks, such as conformationally restricted β-amino acid moieties, into the peptide sequence. Accordingly, the synthesis and incorporation of such conformationally rigid systems into novel type of peptides has gained large interest. Our research group has designed highly efficient methods for the construction of potential antimicrobial peptides. Moreover, a number of synthetic approaches have been developed for the synthesis of various pharmacologically interesting cyclic β-amino acid derivatives as monomers with multiple stereogenic centers.

摘要

在过去的十年中,基于肽的药物研究在药物化学领域受到了高度关注。对于药物设计,为了提高蛋白水解稳定性,理想情况下是将非天然的构建块(如构象受限的β-氨基酸部分)纳入肽序列中。因此,将这种构象刚性系统合成并引入新型肽中引起了广泛关注。我们的研究小组设计了高效的方法来构建潜在的抗菌肽。此外,还开发了许多合成方法来合成各种具有多个立体中心的具有药理活性的环状β-氨基酸衍生物作为单体。

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