Patent ID: 6034211
Filing Date: 2000-03-07
Classification: A61K,C07D,C07F,C07K,C12N

Abstract:
A .beta.-sheet nucleating peptidomimetic, comprising(a) a diarylheterocycle of the formula II: ##STR11## or the formula III: ##STR12## wherein Z is O, S, or NR.sub.a, R.sub.a being C.sub.1-6 alkyl; (b) a recognition strand of between 3 and 21 amino acid residues, said strand comprisinga recognition sequence of a target protein which requires self-assembly for function,a first flanking amino acid residue r.sup.1 selected from histidine and hydrophobic amino acids, wherein r.sup.1 is between said recognition sequence and said diarylheterocycle, and is linked to said diarylheterocycle by an amide bond, anda first N-methylated residue adjacent to an intramolecularly hydrogen-bonded residue; and(c) a blocking strand of between 3 and 21 amino acid residues, said strand comprisinga residue selected from valine, leucine, and isoleucine,a second flanking amino acid residue b.sup.1 selected from histidine and hydrophobic amino acids, wherein said flanking residue is between said blocking strand and said diarylheterocycle, and is linked to said diarylheterocycle by an amide bond, anda second N-methylated residue adjacent to an intramolecularly hydrogen-bonded residue.