[Show abstract][Hide abstract]ABSTRACT: A series of amino acid anthranilamide derivatives identified from a high-throughput screening campaign as novel, potent, and glucose-sensitive inhibitors of human liver glycogen phosphorylase a are described. A solid-phase synthesis using Wang resin was also developed which provided efficient access to a variety of analogues, and resulted in the identification of key structure-activity relationships, and the discovery of a potent exemplar (IC(50)=80 nM). The SAR scope, synthetic strategy, and in vitro results for this series are presented herein.
Article · Aug 2008 · Bioorganic & medicinal chemistry letters
[Show abstract][Hide abstract]ABSTRACT: A series of 3-phenyl-2-propenamides discovered from a high-throughput screening campaign as novel, potent, glucosesensitive inhibitors of human liver glycogen phosphorylase a is described. A solid-phase synthesis on DMHB resin was also developed which provided efficient access not only to certain analogues that could not be cleanly made using more traditional means, but also to a variety of additional analogues. The SAR scope and synthetic strategy are presented herein. (c) 2006 Elsevier Ltd. All rights reserved.
Article · Dec 2006 · Bioorganic & Medicinal Chemistry Letters