CAS: 850664-21-0; N-(3-((2-(4-Amino-1,2,5-Oxadiazol-3-yl)-1-Ethyl-1H-Imidazo[4,5-C]Pyridin-6-yl)Oxy)Phenyl)-4-(2-Morpholinoethoxy)Benzamide

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4-{6-[(3-aminophenyl)oxy]-1-ethyl-1H-imidazo[4,5-c]pyridin-2-yl}-furazan-3-amine 4-chloro-2-hydroxy-5-nitropyridine 2-chloro-N-ethyl-5-nitro-4-pyridinamine N-(3-{[5-amino-4-(ethylamino)-2-pyridinyl]oxy}phenyl)-4-methylbenzenesulfonamide

📜4-羟基-3-硝基吡啶置于palladium On Activated Charcoal 吡啶,盐酸,叔丁基过氧化氢,硫酸,Potassium Tert-Butylate,氢气,羟胺,Potassium Carbonate,溶剂黄146,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺,Sodium Nitrite,三氯氧磷体系中,用 四氢呋喃,1,4-二氧六环,甲醇,癸烷,二氯甲烷,氨,水,重水,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,-35.0~110.0 °C,500.0 Kpa 条件下,反应 109.0H,反应生成 N-[3-[[2-(4-氨基呋咱-3-基)-1-乙基-1H-咪唑并[4,5-C]吡啶-6-基]氧]苯基]-4-[[2-(4-吗啉基)乙基]氧]苯甲酰胺
参考文献:Discovery Of Aminofurazan-Azabenzimidazoles As Inhibitors Of Rho-Kinase With High Kinase Selectivity And Antihypertensive Activity
标题:Discovery Of Aminofurazan-Azabenzimidazoles As Inhibitors Of Rho-Kinase With High Kinase Selectivity And Antihypertensive Activity
摘要:The Discovery,Proposed Binding Mode,And Optimization Of A Novel Class Of Rho-Kinase Inhibitors Are Presented. Appropriate Substitution On The 6-Position Of The Azabenzimidazole Core Provided Subnanomolar Enzyme Potency In Vitro While Dramatically Improving Selectivity Over A Panel Of Other Kinases. Pharmacokinetic Data Was Obtained For The Most Potent And Selective Examples And One (6N) Has Been Shown To Lower Blood Pressure In A Rat Model Of Hypertension.
DOI:10.1021/jm060873P