A series of 3-phenyl-2-propenamides discovered from a high-throughput screening campaign as novel, potent, glucose-sensitive 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 ...
[Berkhout, Theo A.; Blaney, Frank E.; Bridges, Angela M.; Cooper, David G.; Forbes, Ian T.; Gribble, Andrew D.; Groot, Pieter H. E.; Hardy, Adam; Ife, Robert J.; Kaur, Rejbinder; Moores, Kitty E.; Shillito, Helen; Willetts, Jennifer; Witherington, Jason Journal of Medicinal Chemistry, 2003 , vol. 46, # 19 p. 4070 - 4086]
[Berkhout, Theo A.; Blaney, Frank E.; Bridges, Angela M.; Cooper, David G.; Forbes, Ian T.; Gribble, Andrew D.; Groot, Pieter H. E.; Hardy, Adam; Ife, Robert J.; Kaur, Rejbinder; Moores, Kitty E.; Shillito, Helen; Willetts, Jennifer; Witherington, Jason Journal of Medicinal Chemistry, 2003 , vol. 46, # 19 p. 4070 - 4086]