Selective 3- and 6-OH modification of （-）-clausenamide
Selective 3- and 6-OH modification of （-）-clausenamide
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DOI：
10.1016/j.cclet.2011.01.026
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发表时间：
2011-07
影响因子：
9.1
通讯作者：
J. Xue;Xiao Ming Yu
中科院分区：
文献类型：
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作者：
J. Xue;Xiao Ming Yu
（−）-黄皮酰胺是一种正在进行I期临床试验的候选药物，用于治疗阿尔茨海默病（AD）。为了阐明取代基相关的构效关系，设计了6个单取代基修饰的（−）-黄皮酰胺类似物，并通过选择性3-和6-羟基修饰（−）-黄皮酰胺，制备了4个（3-O-甲基、6-O-甲基、3-脱羟基和6-脱羟基）类似物。
(−)-Clausenamide is a drug candidate under Phase I clinical trial for treatment of Alzheimer's disease (AD). In order to elucidate the substituent related structure–activity relationship, six one-substituent modified (−)-clausenamide analogues were designed, and four of them, namely 3-O-methyl, 6-O-methyl, 3-des-hydroxyl and 6-des-hydroxyl analogues were prepared by selective 3- and 6-OH modification of (−)-clausenamide.