CAS: 116247-92-8; 1-(Pyrimidin-2-yl)Piperidin-4-One

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893755-98-1 1344305-03-8 914347-64-1

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CAS号1722-12-9 2-氯嘧啶 | CAS号41979-39-9 4-氧代哌啶酮盐酸盐 | CAS号40064-34-4 4,4-哌啶二醇盐酸盐 | CAS号893755-98-1 1-(2-嘧啶基)-4-哌啶醇

📜4-哌啶酮缩乙二醇置于盐酸,Palladium Diacetate,Sodium T-Butanolate,2-二环己基磷-2,4,6-三异丙基联苯体系中,用 四氢呋喃,水,甲苯,叔丁醇 用作溶剂,化学反应 8.25H,反应生成1-嘧啶-2-哌啶基-4-酮
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