Abstract
Dipeptide isosteres possessing nonhydrolyzable scaffolds as replacements for scissile peptide bonds represent important constituents in peptidomimetics for medicinal and/or biological use. Among these, (E)-alkene dipeptide isosteres, Xaal-Ψ[(E)-CH=CH]-Xaa2 (1), feature three-dimensional structures closely approximating parent peptide bonds; however, certain intrinsic properties of amide bonds such as dipole interaction and hydrogen bonding are lacking. Therefore, (Z)-fluoro-alkene dipeptide isosteres, Xaal-Ψ[(Z)-CF=CH]-Xaa2 (2), have gained significant attention as potentially superior mimetics to (E)-alkene type isosteres [1] (Figure 1).
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