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. 2007 Apr 15;17(8):2229-32.
doi: 10.1016/j.bmcl.2007.01.100. Epub 2007 Feb 2.

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

Ruslan V Bikbulatov  1 , Feng Yan, Bryan L Roth, Jordan K Zjawiony
Affiliations

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

Ruslan V Bikbulatov et al. Bioorg Med Chem Lett. .

Abstract

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.

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Figures

Figure 1
Figure 1
Salvinorins A and B
Scheme 1
Scheme 1
Synthesis of 2β-chloroderivatives
Scheme 2
Scheme 2
2α-Sulfur analogs of salvinorin A
Scheme 3
Scheme 3
2β-Sulfur analogs of salvinorin A
See this image and copyright information in PMC

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