1. Erythrina Alkaloid Analogues as nAChR Antagonists-A Flexible Platform for Leads in Drug Discovery
- Author
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Sebastian Clementson, Anders A. Jensen, Sergio Armentia Matheu, Rasmus P. Clausen, Jesper L. Kristensen, Emil Märcher Rørsted, Emil Glibstrup, Henrik Pedersen, Paulo Jorge Vieira Vital, and Mikkel Jessing
- Subjects
Natural product ,biology ,010405 organic chemistry ,Stereochemistry ,Drug discovery ,Organic Chemistry ,Indolizines ,Total synthesis ,Receptors, Nicotinic ,010402 general chemistry ,biology.organism_classification ,01 natural sciences ,0104 chemical sciences ,Erythrina alkaloid ,chemistry.chemical_compound ,Nicotinic agonist ,Alkaloids ,chemistry ,Drug Discovery ,Erythrina ,Acetylcholine receptor - Abstract
Erythrina alkaloids and their central nervous system effects have been studied for over a century, mainly due to their potent antagonistic actions at β2-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 β2-containing nAChRs.
- Published
- 2021