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Modular Approach to pseudo-Neoclerodanes as Designer κ-Opioid Ligands
Organic Letters ( IF 4.9 ) Pub Date : 2017-09-14 00:00:00 , DOI: 10.1021/acs.orglett.7b02684
Alexander M. Sherwood 1 , Samuel E. Williamson 1 , Rachel S. Crowley 1 , Logan M. Abbott 1 , Victor W. Day 1 , Thomas E. Prisinzano 1
Affiliation  

Informed by previous semisynthetic work on salvinorin A, a modular total synthesis has been developed capable of producing novel compounds targeting the κ-opioid receptor. The strategy has permitted the deliberate simplification and introduction of functionality about the target molecule to provide access to molecular features on salvinorin A otherwise unattainable by semisynthesis. Using this approach, a potent pseudo-neoclerodane κ-opioid receptor ligand (2) has been realized.

中文翻译:

模块化的方法来-Neoclerodanes作为设计师κ阿片配体

根据先前关于Salvinorin A的半合成研究,已开发出一种模块化的全合成产品,能够产生靶向κ阿片受体的新型化合物。该策略允许故意简化和引入有关目标分子的功能,以提供Salvinorin A上分子特征的访问途径,否则半合成是无法实现的。使用这种方法,已经实现了有效的假-新环戊烷κ-阿片样物质受体配体(2)。
更新日期:2017-09-14
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