Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective κ-opioid receptor agonists.
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective κ-opioid receptor agonists.
复制标题
2-烷基-2-甲氧基甲基-salvinorin 醚作为选择性γ-阿片受体激动剂的合成和生物学评价。
DOI：
10.1016/j.bmcl.2015.06.092
复制
发表时间：
2015
影响因子：
2.7
通讯作者：
Liu-Chen,Lee-Yuan
中科院分区：
文献类型：
--
作者：
Lee,DavidYW;Deng,Gang;Ma,Zhongze;Xu,Wei;Yang,Lu;Liu,Jing;Dai,Ronghua;Liu-Chen,Lee-Yuan
The synthesis of a new series of C-2-alkyl-2-methoxymethyl-salvinorin ethers and their binding affinities atκ-,μ-, andδ-opioid receptors are presented. We have developed a synthesis that enables installation of alkyl-substituents at C-2 while maintaining the integrity of the C-2 methoxymethyl ether and retainingκ-opioid receptor binding activity. Among these new compounds, 2-methyl-2-methoxymethyl-salvinorin ether (9a) is a potent full agonist at theκreceptor and shows comparable potency inKiand EC50with salvinorin A and U50488H. These C2-alkylated analogs have been identified as fullκagonists.
