Erythrina Alkaloid Analogues as nAChR Antagonists-A Flexible Platform for Leads in Drug Discovery

Erythrina alkaloids and their central nervous system effects have been studied for over a century, mainly due to their potent antagonistic actions at beta 2-containing nicotinic acetylcholine receptors (nAChRs). In the present work, we report a synthetic approach giving access to a diverse set of Erythrina natural product analogues and present the enantioselective total synthesis of (+)-Cocculine and (+)-Cocculidine, both found to be potent antagonists of the beta 2-containing nAChRs.

Automated summary

The study presents a synthetic approach for generating a diverse set of Erythrina natural product analogues, as well as the enantioselective total synthesis of (+)-Cocculine and (+)-Cocculidine, both of which were found to be potent antagonists of beta 2-containing nAChRs.