Seite - (000310) - in Biomedical Chemistry: Current Trends and Developments

peptide analogs, in which each amino acid residue of the two target peptides was replaced sequentially with an alanine, was synthesized. In the truncation studies, one amino acid at a time was removed from the N-terminal. Both C-terminal carboxylic acids and carboxamides were included. Figure 3.3.9: Illustration of the modifications of A) SP1–7 and B) EM-2, used in the SAR study. 3.3.2.2.2 Structure–activity Relationship The two lead peptides, SP1–7 (1) and EM-2 (2), the Ala-substituted peptides 3–13, the N- and C-terminally modified analogs 14–16 and 28–29, the truncated analogs 17– 27, and the (d) and (l) variants 30–32 were prepared and biochemically evaluated (Tables 3.3.3 and 3.3.4). Table 3.3.3: Ki values of SP1–7 and EM-2 analogs for inhibition of [3H]-SP1–7 binding to rat spinal cord membrane.