| 摘要 |
The compounds of the invention are generally described by the formula: <?in-line-formulae description="In-line Formulae" end="lead"?>B<SUB>1</SUB>Z*<SUB>2</SUB>B<SUB>3</SUB>Z*<SUB>4</SUB>X*<SUB>5</SUB>Q<SUB>6</SUB>F<SUB>7</SUB>X<SUB>8</SUB>X<SUB>9</SUB>X<SUB>10</SUB>X<SUB>11</SUB>, (1)<?in-line-formulae description="In-line Formulae" end="tail"?> <?in-line-formulae description="In-line Formulae" end="lead"?>B<SUB>1</SUB>X<SUB>2</SUB>X<SUB>3</SUB>X<SUB>4</SUB>X<SUB>5</SUB>Q<SUB>6</SUB>F<SUB>7</SUB>X<SUB>8</SUB>X<SUB>9</SUB>X<SUB>10</SUB>X<SUB>11</SUB>, or (2)<?in-line-formulae description="In-line Formulae" end="tail"?> <?in-line-formulae description="In-line Formulae" end="lead"?>B<SUB>1</SUB>Z<SUB>2</SUB>B<SUB>3</SUB>X<SUB>4</SUB>Z<SUB>5</SUB>Q<SUB>6</SUB>F<SUB>7</SUB>Z<SUB>8</SUB>X<SUB>9</SUB>X<SUB>10</SUB>X<SUB>11</SUB> (3)<?in-line-formulae description="In-line Formulae" end="tail"?> 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 of 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 of 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. |
