Design of a novel secondary structure scaffolding device: Induction of a reverse turn in tetrapeptides by incorporating a β-amino acid and stereocontrolled free radical α-substitution reactions in peptide motifs
The incorporation of α-substituted β-amino acids into a tetrapeptide motif induces a reverse rum in aprotic solvent systems as revealed by NOESY and ROESY techniques, and by CD spectra. The conformations of these compounds have been studied by molecular modeling, and further supported by performing a highly stereoselective free radical allylation reaction on an α-phenylseleno β-amino acid unit within the tetrapeptide.
Hanessian, Stephen,Yang, Hua
p. 3155 - 3158
(2007/10/03)
Peptidase inhibitors
This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
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(2008/06/13)
NEW SYNTHESIS OF PEPTIDE SUBSTRATES AND INHIBITORS OF HUMAN GRANULOCYTE ELASTASE
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Martynov, V. F.,Leont'eva, L. I.,Sorochinskaya, E. I.,Smirnov, A. O.
p. 384 - 388
(2007/10/02)
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