4.8 Article

Three-Dimensional Structural Diversity-Oriented Peptidomimetics Based on the Cyclopropylic Strain

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ORGANIC LETTERS
卷 15, 期 7, 页码 1686-1689

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AMER CHEMICAL SOC
DOI: 10.1021/ol400469w

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资金

  1. Japan Society for the Promotion of Science [21390028, 2310550201, 2179000300]
  2. Grants-in-Aid for Scientific Research [23246013, 24390023, 24710260, 25105702] Funding Source: KAKEN

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Conformationally restricted peptidomimetics comprising eight stereoisomeric scaffolds with three-dimensional structural diversity were designed based on the structural features of cyclopropane, that is, cyclopropylic strain, which mimic wide-ranging tetrapeptide conformations covering beta-turns through beta-strands. Stereoselective synthesis of the designed peptidomimetics led to the identification of nonpeptidic melanocortin-4 receptor ligands.

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