3-甲氧基-苯肼置于sodium Acetate,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,水 用作溶剂,化学反应生成6-甲氧基吲哚-2-羧酸
参考文献:Structure-Based Design And Biological Evaluation Of Novel 2-(Indol-2-yl) Thiazole Derivatives As Xanthine Oxidase Inhibitors
标题:Structure-Based Design And Biological Evaluation Of Novel 2-(Indol-2-yl) Thiazole Derivatives As Xanthine Oxidase Inhibitors
摘要:Inhibition Of Xanthine Oxidase (Xo) Has Obviously Been A Central Concept For Controlling Hyperuricemia,Which Causes Serious And Painful Inflammatory Arthritis Disease Such As Gout. We Discovered A Series Of Novel 2-(Indol-2-yl) Thiazole Derivatives As Xo Inhibitors At The Level Of Nanomolar Activity. Structure-Guided Design Using Molecular Modeling Program (Accelrys Software Program) Provided An Excellent Basis For Optimization Of 2-(Indol-2-yl) Thiazole Compounds. Structure-Activity Relationship Indicated That Hydrophobic Alkoxy Group (Isopropoxy,Cyclopentoxy) At 5-Position And Hydrogen Binding Acceptor (No2,Cn) At 7-Position Of Indole Ring Appear As Critical Functional Groups. Among The Compounds,2-(7-Nitro-5-Isopropoxy-Indol-2-yl)-4-Methylthiazole-5-Carboxylic Acid (9M) Exhibits The Most Potent Xo Inhibitory Activity (Ic50 Value: 5.1 Nm) And The Excellent Uric Acid Lowering Activity In Potassium Oxonate Induced Hyperuricemic Rat Model. (C) 2016 Published By Elsevier Ltd.
Doi:10.1016/j.Bmcl.2015.12.055