Medicinal Chemistry Endeavors around the Phytocannabinoids

AbstractOver the past 50 years, a considerable research in medicinal chemistry has been carried out around the natural constituents ofCannabis sativaL. Following the identification of Δ9‐tetrahydrocannabinol (Δ9‐THC) in 1964, critical chemical modifications,e.g., variation of the side chain at C(3) and the opening of the tricyclic scaffold, have led to the characterization of potent and cannabinoid receptor subtype‐selective ligands. Those ligands that demonstrate high affinity for the cannabinoid receptors and good biological efficacy are still used as powerful pharmacological tools. This review summarizes past as well as recent developments in the structure–activity relationships of phytocannabinoids.