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

Sebastian ClementsonSergio Armentia MatheuEmil Märcher RørstedHenrik PedersenAnders A JensenRasmus Prætorius ClausenPaulo VitalEmil GlibstrupMikkel JessingJesper L Kristensen
Published in: The Journal of organic chemistry (2021)
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.
Keyphrases
  • drug discovery
  • molecular docking
  • anti inflammatory
  • structure activity relationship
  • high throughput
  • solid state