Medicinal chemistry endeavors around the phytocannabinoids.
Over the past 50 years, a considerable research in medicinal chemistry has been carried out around the natural constituents of Cannabis sativa L. Following the identification of Delta9-tetrahydrocannabinol (Delta9-THC) in 1964, critical chemical modifications, e.g., variation of the side chain at C3 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.
Stern
Eric
E
Drug Design and Discovery Center and Unité de Chimie pharmaceutique et de Radiopharmacie, Ecole de Pharmacie, Faculté de Médecine, Université catholique de Louvain, Avenue E. Mounier 73, U.C.L. 73.40, B-1200 Bruxelles.
Lambert
Didier M
DM
D000818:Animals; D002186:Cannabinoids / Q000737:chemistry* / Q000302:isolation & purification; D002626:Chemistry, Pharmaceutical; D006801:Humans; D008024:Ligands; D051379:Mice; D010946:Plants, Medicinal / Q000737:chemistry*; D051381:Rats; D043882:Receptors, Cannabinoid / Q000187:drug effects*; D013329:Structure-Activity Relationship
D002186:Cannabinoids; D008024:Ligands; D043882:Receptors, Cannabinoid