| 摘要 |
The invention relates to compounds of formula (I) or (II), which are of interest especially for inhibition of polymerization of amyloid beta peptide, as model substances for synthesis of amyloid beta peptide-ligands, as tools for the identification of other organic compounds with similar functional properties and/or as ligands for detection of amyloid deposits using e.g., positron emission tomography (PET). Formula (II) is: R1-A'-Y'-Leu-X'-Z'-B'-R2 in which X' means any group or amino acid imparting to the compound according to formula (I) the ability to bind to the KLVFF-sequence in amyloid beta peptide, or two amino acids imparting the same ability, but with the proviso that one is not proline; Y' means any amino acid; Z' means any non-acidic amino acid; A' means a direct bond or an alpha-amino acid bonded at the carboxyl terminal of the alpha-carboxy group or a di-, tri-, tetra- or pentapeptide bonded at the carboxyl terminal of the alpha-carboxy group; B' means a direct bond or an alpha-amino acid bonded at the alpha-nitrogen or a di-, tri-, tetra- or pentapeptide bonded at the alpha-nitrogen of the N-terminal alpha-amino acid; R1 is H or -CO-R3 bonded at the alpha-amino group of A'; R2 is H, -OR4 or NR5R6, all bonded to the alpha-carboxyl group of the alpha-carboxyterminal of B'; R3 and R4 are straight or branched carbon chain of 1-4 carbon atoms; R5 and R6 are independently H, alkyl, cycloalkyl, aryl or substituted aryl or together are -(CH2)n- where n is 4-5; and R1 and R2 together can form a hydrocarbon ring of heterocyclic ring; all alpha-amino acids being either D- or L-isomers.
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