Salvinorins A和B的2-硫代类似物的简便合成及其体外药理活性
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
作者信息
Bikbulatov Ruslan V, Yan Feng, Roth Bryan L, Zjawiony Jordan K
机构信息
Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA.
出版信息
Bioorg Med Chem Lett. 2007 Apr 15;17(8):2229-32. doi: 10.1016/j.bmcl.2007.01.100. Epub 2007 Feb 2.
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.
为了研究药物与受体的相互作用，合成了具有极强活性的天然κ-阿片受体（KOR）激动剂萨尔维诺林A的新型硫代衍生物。对所获得的化合物进行了受体结合亲和力检测。在碳原子C-2处具有与天然萨尔维诺林A相同构型的类似物对KOR的亲和力高于其相应的差向异构体。
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