Tethered Libraries:  Solid-Phase Synthesis of Substituted Urea-Linked Bicyclic Guanidines

2001 ◽  
Vol 3 (2) ◽  
pp. 189-195 ◽  
Author(s):  
Achyuta N. Acharya ◽  
Adel Nefzi ◽  
John M. Ostresh ◽  
Richard A. Houghten
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis ◽  
Substituted Urea

Synthesis and Screening of A DNA-Encoded Library of Non-Peptidic Macrocycles

2020 ◽  
Author(s):  
Eric Koesema ◽  
Animesh Roy ◽  
Nicholas G. Paciaroni ◽  
Thomas Kodadek
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Cell Permeability ◽  
Phase Synthesis ◽  
Protein Ligands ◽  
High Affinity ◽  
Scaffold Diversity

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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