Solid-Phase Synthesis of Aspartic Peptidase Inhibitors:  3-Alkoxy-4-Aryl Piperidines

2001 ◽  
Vol 3 (17) ◽  
pp. 2625-2628 ◽  
Author(s):  
Matthew G. Bursavich ◽  
Daniel H. Rich



2020 ◽  
Author(s):  
Eric Koesema ◽  
Animesh Roy ◽  
Nicholas G. Paciaroni ◽  
Thomas Kodadek

There is considerable interest in the development of libraries of non-peptidic macrocycles as a source of ligands for difficult targets. We report here the solid-phase synthesis of a DNA-encoded library of several hundred thousand thioether-linked macrocycles. The library was designed to be highly diverse with respect to backbone scaffold diversity and to minimize the number of amide N-H bonds, which compromise cell permeability. The utility of the library as a source of protein ligands is demonstrated through the isolation of compounds that bind streptavidin, a model target, with high affinity.



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