Synthesis and Biological Evaluation of O6C-Salvinorin Alkyne Probes
Etienne Cotter, Giovanni Leoni, Nathan Dao et al.
The salvinorins represent a unique class of polyoxygenated, non-nitrogenous diterpenes that potently and selectively modulate the kappa-opioid receptor (KOR). We recently disclosed a de novo asymmetric synthesis of this scaffold that enabled the discovery of highly potent, biased analogs, including C11-alkynes designed for the CATCH (Clearing-Assisted Tissue Click Chemistry) assay. Here, we...