| abstract |
Peptide inhibitors of serine proteases, especially thrombin, in which the P1-P2 natural amide linkage is replaced by another bond. Exemplary thrombin inhibitors are of the formula: X-(aa3)-(aa2)-γ-(aa1)-Z wherein X is H or a substituent on the N-terminal amino group, aa3 is a hydrophobic amino acid such as Phe, aa2 is Pro, aa1 is Arg or an Arg analogue such as methoxypropylglycyl, Z is -COOH or a heteroatom acid group, such as boronate, or a derivative of either, and Γ is a non-amide linkage, typically containing up to 5 in-chain atoms, such as -CO¿2?-, -CH2O-, NHCO- or -CH2-CH2-. |