CAS: 17899-49-9; 5-Ethyl-4H,5H,6H,7H-[1,3]Thiazolo[5,4-C]Pyridin-2-Amine

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N-ethyl-4-piperidone CYANAMID

N-乙基-4-哌啶酮,氰胺置于四氢吡咯,Sulfur体系中,用 异丙醇 用作溶剂,化学反应 8.0H,以59%的收率获得5-乙基-4,5,6,7-四氢噻唑并[5,4-C]吡啶-2-胺
参考文献:Discovery Of Cycloalkyl-Fused N-Thiazol-2-Yl-Benzamides As Tissue Non-Specific Glucokinase Activators: Design,Synthesis,And Biological Evaluation
标题:Discovery Of Cycloalkyl-Fused N-Thiazol-2-Yl-Benzamides As Tissue Non-Specific Glucokinase Activators: Design,Synthesis,And Biological Evaluation
摘要:Glucokinase (Gk) Activators Are Being Developed For The Treatment Of Type 2 Diabetes Mellitus (T2Dm). However,Existing Gk Activators Have Risks Of Hypoglycemia Caused By Over-Activation Of Gk In Islet Cells And Dyslipidemia Caused By Over-Activation Of Intrahepatic Gk. In The Effort To Mitigate Risks Of Hypoglycemia And Dyslipidemia While Maintaining The Promising Efficacy Of Gk Activator,We Investigated A Series Of Cycloalkyl-Fused N-Thiazol-2-Yl-Benzamides As Tissue Non-Specific Partial Gk Activators,Which Led To The Identification Of Compound 72 That Showed A Good Balance Between In Vitro Potency And Enzyme Kinetic Parameters,And Protected Beta-Cells From Streptozotocin-Induced Apoptosis. Chronic Treatment Of Compound 72 Demonstrated Its Potent Activity In Regulation Of Glucose Homeostasis And Low Risk Of Dyslipidemia With Diabetic Db/db Mice In Oral Glucose Tolerance Test (Ogtt). Moreover,Acute Treatment Of Compound 72 Did Not Induce Hypoglycemia In C57Bl/6J Mice Even At 200 Mg/kg Via Oral Administration. (C) 2017 Elsevier Masson Sas. All Rights Reserved.
Doi:10.1016/j.Ejmech.2017.07.051