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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >Betidamino acids: Versatile and constrained scaffolds for drug discovery
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Betidamino acids: Versatile and constrained scaffolds for drug discovery

机译:Betid氨基酸:用于药物发现的多功能和受限支架

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摘要

Betidamino acids (a contraction of "beta" position and "amide") are N'-monoacylated (optionally, N'- monoacylated and N-mono- or N,N'-dialkylated) aminogly- cine derivatives in which each N'-acyl/alkyl group may mimic naturally occurring amino acid side chains or introduce novel functionalities. Betidamino acids are most conveniently gen- erated on solid supports used for the synthesis of peptides by selective acylation of one of the two amino functions of orthogonally protected aminoglycine(s) to generate the side chain either prior to or after the elongation of the main chain.
机译:Betid氨基酸(“β”位置和“酰胺”的收缩)是N'-单酰化(可选地,N'-单酰化和N-单-或N,N'-二烷基化)氨基甘氨酸衍生物,其中每个N'-酰基/烷基可以模拟天然存在的氨基酸侧链或引入新的功能。最适合在肽合成所用的固体支持物上生成双歧氨基酸,方法是在延长主链之前或之后,将正交保护的氨基甘氨酸的两个氨基官能团之一进行选择性酰化,以生成侧链。

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