| 摘要 |
<p>Compounds termed 'betides' mimic peptides and contain one or more residues of aminoglycine, Cα-aminoalanine, aminosarcosine or the like wherein the side chain amino group has been acylated and optionally also alkylated. Generally, betides have the formula: X¿N?-X1-X2-X3-Xm-X4-X5-X6-XC, where XN is an acyl or other N-terminal group or a peptide up to about 50 amino acids in length having such a group; XC is OH, NH2 or other C-terminal group or a peptide up to about 50 amino acids in length having such a group; and X1-X6 are each independently a betidamino acid or α-amino acid or des-X; and Xm is a peptide up to about 50 amino acids or des-X; provided however that at least one of X1-X6 is a betidamino acid residue having formula (I), wherein Ro is H or CH3, R and R2 are H or lower alkyl, and R3 is an acyl group, an isocyanate or isothiocyanate group, a sulfonyl group or the like. To make a betide, an aminoglycine residue is subjected to side chain acylation, and optionally also alkylation, after it is coupled into a peptide intermediate. By synthesizing betides with multiples substituents at one or more positions in an otherwise peptidic chain, efficient screening of betides which mimic peptides having a large number of different natural or unnatural amino acid substituents at a particular position, and optionally both D- and L-isomers thereof, is possible.</p> |
