Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A
Graphical abstract
We have carried out the synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A. SAR studies suggest that electronic factors that may affect either the electron density of hydrogen bond acceptor at C-12 or hydrophobic interactions between C-12 moiety and KOPR are critical to salvinorin A templated C-12 analog’s affinity for KOPR.
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Acknowledgments
We thank Dr. Yongxuan Su of University of California, San Diego for HR-MS measurements of all samples and National Institutes of Health for financial support (RO1DA019688).
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