Synthesis and biological evaluation of new salvinorin A analogues incorporating natural amino acids.
Bioorganic & Medicinal Chemistry Letters(2011)
摘要
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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关键词
Salvia divinorum,Salvinorin B,Neoclerodane diterpenoid,Natural amino acids,Opioid receptor ligands
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