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📜6-甲基-N-硝基-2-吡啶胺置于硫酸体系中,化学反应生成2-氨基-3,5-二硝基-6-甲基砒啶
参考文献:Synthesis And Biological Evaluation Of Aroylguanidines Related To Amiloride As Inhibitors Of The Human Platelet Na+/h+ Exchanger
标题:Synthesis And Biological Evaluation Of Aroylguanidines Related To Amiloride As Inhibitors Of The Human Platelet Na+/h+ Exchanger
摘要:Pyridine And Benzene Bioisosteres Of Amiloride Were Synthesized And Evaluated For Their Inhibitory Potency Against The Sodium-Hydrogen Exchanger (Nhe) Involved In Intracellular Ph Regulation. The Inhibition Of Nhe Was Determined By Using The Platelet Swelling Assay (Psa) In Which The Swelling Of Human Platelets Was Induced By Their Incubation In An Acid Buffer (Ph 6.7). Additionally,The Inhibitory Potency Of The Most Active Compounds Was Assessed By Measuring The Inhibition Of The Eipa-Sensitive Na-22 (+) Uptake (Uia) By Human Platelets After Intracellular Acidosis. The Results Indicated That Several Benzene Derivatives And Compounds Bearing An Carbonylguanidine Moiety In The Meta Position Of The Pyridine Nitrogen Were Much More Potent Than Amiloride (Psa:Ic50 = 43.5 Mum,Uia:Ic50 = 100.1 Mum),But Less Than Eipa,A Pyrazine Nhe Inhibitor (Psa:Ic50=0.08 Mum,Uia: Ic50-0.5 Mum). In Both Biological Assays (2-Amino-5-Bromo-Pyridine-3-Carbonyl)Guanidine (32) Was The Most Active Molecule (Psa: Ic50 = 0.8 Mum,Uia : Ic50 = 0.8 Mum). Our Investigations Demonstrated That The Replacement Of The Pyrazine Ring Of Amiloride E By A Pyridine Ora Phenyl Ring Improved The Nhe Inhibitory Potency (Phenyl >Pyridine >Pyrazine). (C) 2002 Elsevier Science Ltd. All Rights Reserved.
Doi:10.1016/s0968-0896(02)00022-6