Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B

被引：23
|
作者：
Blkbulatov, Ruslan V.
Yan, Feng
Roth, Bryan L.
Zjawiony, Jordan K. [1 ]
机构：
[1] Univ Mississippi, Sch Pharm, Dept Pharmacognosy, University, MS 38677 USA
[2] Univ N Carolina, Dept Pharmacol, Sch Med, Chapel Hill, NC 27599 USA
[3] Univ N Carolina, Div Med Chem & Nat Prod, Sch Pharm, NIMH Psychoact Drug Screening Program, Chapel Hill, NC 27599 USA
[4] Univ Mississippi, Sch Pharm, Pharmaceut Sci Res Inst, Natl Ctr Nat Prod Res, University, MS 38677 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 08期
关键词：
kappa-opioid receptors agonists; semi-synthesis; salvinorin A and B thioderivatives;
D O I：
10.1016/j.bmcl.2007.01.100
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：2229 / 2232
页数：4
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