The compounds of the invention are generally described by the formula (1):
B.sub.1Z*.sub.2B.sub.3Z*.sub.4X*.sub.5Q.sub.6F.sub.7X.sub.8X.sub.9X.sub.1-
0X.sub.11, (2):
B.sub.1X.sub.2X.sub.3X.sub.4X.sub.5Q.sub.6F.sub.7X.sub.8X.sub.9X.sub.10X.-
sub.11, or (3):
B.sub.1X.sub.2B.sub.3X.sub.4Z.sub.5Q.sub.6F.sub.7Z.sub.8X.sub.9X.sub.10X.-
sub.11 and the salts, esters, amides, and acyl forms thereof. Each
position represented by a letter indicates a single amino acid residue: B
is a basic or polar/large amino acid or a modified form thereof; X is a
small or hydrophobic amino acid or a modified form thereof; X* is a small
or polar/large amino acid or a modified form thereof; Z is a polar/large
or hydrophobic amino acid or a modified form thereof; Z* is Proline or a
polar/large or hydrophobic amino acid or a modified form thereof. As
described below, one or more of the peptide linkages between the amino
acid residues may be replaced by a peptide linkage mimic. These compounds
may be used as molecular building blocks to create compounds that are
optimized for inhibiting the protease activity of Botulinum B and tetanus
toxins.