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Short synthesis of a novel class of salvinorin A analogs with hemiacetalic structure |
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| Authors: | Ruslan V Bikbulatov Wentao Jin Bryan L Roth Jordan K Zjawiony |
| Institution: | a Department of Phamacognosy, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA b Department of Pharmacology, School of Medicine and Division of Medicinal Chemistry and Natural Products, School of Pharmacy, NIMH Psychoactive Drug Screening Program, University of North Carolina, Chapel Hill, NC 27599, USA c National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA |
| Abstract: | Novel semisynthetic analogs of salvinorin A, a full agonist having extraordinary affinity as well as selectivity for the κ-opioid receptor (KOR), were obtained in good yields. The derivatives are remarkable for their unusual and unique hemiacetal structure in the salvinorin series of compounds. The formation of the hemiacetal occurs with epimerization at C-12, thus preserving the original configuration of salvinorin A. The dimethyl ester derivative of the hemiacetal was found to have an affinity for both KOR and MOR (μ-opioid receptor). |
| Keywords: | Salvinorin A KOR ligands Hemiacetal Dual affinity |
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