Saturated bioisosteres of benzene: where to go next?

被引：261
|
作者：
Mykhailiuk, Pavel K. [1 ,2 ]
机构：
[1] Enamine Ltd, Chervonotkatska 78, UA-02094 Kiev, Ukraine
[2] Taras Shevchenko Natl Univ Kyiv, Chem Dept, Volodymyrska 64, UA-01601 Kiev, Ukraine
来源：
ORGANIC & BIOMOLECULAR CHEMISTRY | 2019年 / 17卷 / 11期
关键词：
BIOLOGICAL EVALUATION; LABEL; ACID; CUBANES; DESIGN; CHEMISTRY; DISCOVERY; PROTOCOL; PEPTIDE; BINDING;
D O I：
10.1039/c8ob02812e
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
The replacement of para-substituted benzenes with saturated bi- and polycyclic bioisosteres - bicyclo[1.1.1]pentane, bicyclo[2.2.2]octane and cubane, - often increases the potency, selectivity and metabolic stability of bioactive compounds. The currently remaining challenge for chemists, however, is to rationally design, synthesize and validate the saturated bioisosteres for ortho-and meta-substituted benzenes.
引用
收藏
页码：2839 / 2849
页数：11
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