Efficient microwave-assisted synthesis of multivalent dendrimeric peptides using cycloaddition reaction (click) chemistry

摘要

Multivalent dendrimeric peptides were synthesized via a microwave-assisted Huisgen 1,3-dipolar cycloaddition between azido peptides and dendrimeric alkynes in yields ranging from 46 to 96%.Dendrimers are versatile constructs for the simultaneous presentation of especially biologically relevant ligands.These multivalent constructs are especially interesting for enhancing the interaction of weakly interacting individual ligands e.g.carbohydrates.We have successfully explored this in the design,synthesis and biological evaluation of dendrimeric carbohydrates.In addition,dendrimers might serve as promising molecular scaffolds for increasing effects merely by offering a number of ligands or by aliening these liaands.