2. Academic Validation
  3. Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids

Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):160-3. doi: 10.1016/j.bmcl.2010.11.046.
Jakub Fichna 1,  Kevin Lewellyn,  Feng Yan,  Bryan L Roth,  Jordan K Zjawiony
Affiliations

Affiliation

  • 1 Department of Pharmacognosy and Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, MS38677-1848, USA.
PMID: 21115248 DOI: 10.1016/j.bmcl.2010.11.046
Abstract

The synthesis and in vitro evaluation of a new series of salvinorin A analogues substituted at the C(2) position with natural Amino acids is reported. Compound 12, containing Val, displayed high affinity and full agonist activity at the kappa-opioid receptor. Analogues with bulky and/or aromatic residues were inactive, showing the importance of size and electronegativity of C(2)-substituents for binding affinity of salvinorin A derivatives.

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