Synthesis and structure–activity relationships of 3-phenyl-2-propenamides as inhibitors of glycogen phosphorylase a

…, M Patel, J Gale, H Li, F Tavares, SA Thomson

Index: Li, Yue H.; Coppo, Frank T.; Evans, Karen A.; Graybill, Todd L.; Patel, Mehul; Gale, Jennifer; Li, Hu; Tavares, Francis; Thomson, Stephen A. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 22 p. 5892 - 5896

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Citation Number: 9

Abstract

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 ...