📜4-Hydroxymethylphenoxymethyl Polystyrene Resin,Fmoc-L-亮氨酸置于吡啶,2,6-二甲基-苯甲酰氯体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 20.0H,反应生成Fmoc-(R)-2-(2-噻吩基)-甘氨酸
参考文献:Amino Acid Anthranilamide Derivatives As A New Class Of Glycogen Phosphorylase Inhibitors
标题:Amino Acid Anthranilamide Derivatives As A New Class Of Glycogen Phosphorylase Inhibitors
摘要: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. (C) 2008 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2008.05.102