📜在 哌啶体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 0.35H,反应生成(S)-N-Fmoc-α-甲基-2-氟苯丙氨酸
参考文献:Eleven Amino Acid Glucagon-Like Peptide-1 Receptor Agonists With Antidiabetic Activity
标题:Eleven Amino Acid Glucagon-Like Peptide-1 Receptor Agonists With Antidiabetic Activity
摘要:Glucagon-Like Peptide 1 (Glp-1) Is A 30 Or 31 Amino Acid Peptide Hormone That Contributes To The Physiological Regulation Of Glucose Homeostasis And Food Intake. Herein,We Report The Discovery Of A Novel Class Of 11 Amino Acid Glp-1 Receptor Agonists. These Peptides Consist Of A Structurally Optimized 9-Mer,Which Is Closely Related To The N-Terminal 9 Amino Acids Of Glp-1,Linked To A Substituted C-Terminal Biphenylalanine (Bip) Dipeptide. Sar Studies Resulted In 11-Mer Glp-1R Agonists With Similar In Vitro Potency To The Native 30-Mer. Peptides 21 And 22 Acutely Reduced Plasma Glucose Excursions And Increased Plasma Insulin Concentrations In A Mouse Model Of Diabetes. These Peptides Also Showed Sustained Exposures Over Several Hours In Mouse And Dog Models. The Described 11-Mer Glp-1 Receptor Agonists Represent A New Tool In Further Understanding Glp-1 Receptor Pharmacology That May Lead To Novel Antidiabetic Agents.
Doi:10.1021/jm900752A