Stable analogs of disulfide bond-containing bioactive peptides

摘要

(57) I disclose a stable cyclic peptide analogues containing [summary] disulfide bond. This disulfide bond is modified in one of four ways. (A) sulfide shrinkage, (b) the distribution of substitution, (c) or thioketal extension, they are (d) alkylation extension. In sulfide contraction, is replaced monosulfide bond (-S-) is disulfide bond (-S-S-), chemotactic agents or ligands such as 2-functional effector molecule to bind to the new peptide chain. The isosteres substitutions, one sulfur atom is replaced by a carbon atom, one carbon atom is a bifunctional effector molecule of at least a modified side. The thioketal extended, alkylidene units (-CR ₁ R ₂ -) is inserted between two sulfur atoms. The alkylation extension, not C ₂ alkyl moiety of ₃ C is inserted between two sulfur atoms.