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- W2048705687 abstract "Nucleophilic imine additions with vinyl organometallics have developed into efficient, high-yielding, and robust methodologies to generate structurally diverse allylic amines. We have used the hydrozirconation/transmetalation/imine addition protocol in the synthesis of allylic amine intermediates for peptide bond isosteres, phosphatase inhibitors, and mitochondria-targeted peptide mimetics. The gramicidin S-derived XJB-5-131 and JP4-039 and their analogues have been prepared on up to 160-g scale for preclinical studies. These (E)-alkene peptide isosteres adopt type II′ β-turn secondary structures and display impressive biological properties including selective reactions with reactive oxygen species (ROS) and prevention of apoptosis." @default.
- W2048705687 created "2016-06-24" @default.
- W2048705687 creator A5018024103 @default.
- W2048705687 creator A5059406567 @default.
- W2048705687 creator A5062267549 @default.
- W2048705687 date "2012-01-04" @default.
- W2048705687 modified "2023-10-11" @default.
- W2048705687 title "Allylic Amines as Key Building Blocks in the Synthesis of (<i>E</i>)-Alkene Peptide Isosteres" @default.
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- W2048705687 doi "https://doi.org/10.1021/op2002613" @default.
- W2048705687 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3272643" @default.
- W2048705687 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22323894" @default.
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