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.

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页码：2229 / 2232

页数：4

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