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1, 2, 3-trisubstituted cyclopropanes as conformationally restricted peptide isosteres: application to the design and synthesis of novel renin inhibitors

…, CJ Oalmann, WR Baker, SL Condon…

文献索引:Martin, Stephen F.; Austin, Richard E.; Oalmann, Christopher J.; Baker, William R.; Condon, Stephen L.; et al. Journal of Medicinal Chemistry, 1992 , vol. <10> 35, # 35 p. 1710 - 1721

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被引用次数: 91

摘要

The 1, 2, 3-trisubstituted cyclopropanes 6 and 7 are the first members of a novel class of isosteric replacements for peptide linkages that are more generally represented by the dipeptide mimics 2 and 3. These unique peptide surrogates are specifically designed to lock a section of a peptide backbone in an extended 0-strand conformation (@-angle restriction) while simultaneously enforcing one of two specifically defined orientations for the amino ...