The present work focuses on five objective targets as listed below:
1. Design of disubstituted [1,2,3]-triazolyl-comprising molecular blocks as peptide backbone mimics with locked amide conformation;
2. Development of a valid synthetic approach towards the mentioned triazolyl surrogates with focus on their application in Fmoc-based SPPS;
3. Study of the structure-activity relationship in peptidic molecules using the developed triazolyl blocks on two model systems:
a) the potent protease inhibitor sunflower trypsin inhibitor 1 (SFTI-1[1,14]) and
b) a peptide-based enzyme maquette of nickel superoxide dismutase (Ni(m7-NH2));
4. Study of the structural properties of triazolyl patterns in peptidic molecules using molecular dynamic simulations;
5. Development of a valuable system towards the study of PHIP effects in biomolecules based on model peptides comprising an unsaturated alkyne moiety in their side chains.
Marco Körner