📜2-氯-4-氰基吡啶,乙胺 以 四氢呋喃 作为反应溶剂,化学反应 3.0H,以49%的收率获得产物2-(乙基氨基)-4-吡啶甲腈
参考文献:Discovery Of An N-(2-Aminopyridin-4-Ylmethyl)Nicotinamide Derivative: A Potent And Orally Bioavailable Ncx Inhibitor
标题:Discovery Of An N-(2-Aminopyridin-4-Ylmethyl)Nicotinamide Derivative: A Potent And Orally Bioavailable Ncx Inhibitor
摘要:Ca2+ Overload In Myocardial Cells Is Responsible For Arrhythmia. Sodium-Calcium Exchanger (Ncx) Inhibitors Are More Effective Than Sodium Hydrogen Exchanger (Nhe) Inhibitors With Regard To Modulation Of Ca2+ Overload,Because Ncx Inhibitors Can Directly Inhibit The Influx Of Ca2+ Into Cells. Ncx Is An Attractive Target For The Treatment Of Heart Failure And Ischemia-Reper-Fusion. We Have Designed And Synthesized A Series Of N-(2-Aminopyridin-4-Ylmethyl)Nicotinamide Derivatives,Based On Compound 5. We Have Discovered A Novel Ncx Inhibitor (23H) With An Ic50 Value Of 0.12 Mu M Against Reverse Ncx. The Inhibitory Activities Of Our Ncx Inhibitors Against Cytochrome P450 Were Also Evaluated. The Effects On Heart Failure And The Pharmacokinetic Profile Of Compound 23H Are Discussed. (C) 2005 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2005.03.052