Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B
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DOI：
10.1016/j.bmcl.2007.01.100
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发表时间：
2007-04-15
影响因子：
2.7
通讯作者：
Zjawiony, Jordan K.
中科院分区：
文献类型：
--
作者：
Blkbulatov, Ruslan V.;Yan, Feng;Zjawiony, Jordan K.
为了研究药物-受体相互作用，合成了鼠尾草素A（一种极其有效的天然κ-阿片受体（KOR）激动剂）的新的硫代衍生物。检查所获得的化合物的受体结合亲和力。在碳原子C-2处具有与天然鼠尾草素A中相同构型的类似物显示出比其相应差向异构体更高的对KOR的亲和力。(c)2007爱思唯尔有限公司版权所有。
To study drug-receptor interactions, new thio-derivatives of salvinorin A, an extremely potent natural kappa-opioid receptor (KOR) agonist, were synthesized. Obtained compounds were examined for receptor binding affinity. Analogs with the same configuration at carbon atom C-2 as in natural salvinorin A showed higher affinity to KOR than their corresponding epimers. (c) 2007 Elsevier Ltd. All rights reserved.