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

Clementson, Sebastian LU orcid ; Matheu, Sergio Armentia ; Rørsted, Emil Märcher ; Pedersen, Henrik ; Jensen, Anders A. ; Clausen, Rasmus P. ; Vital, Paulo ; Glibstrup, Emil ; Jessing, Mikkel and Kristensen, Jesper L. (2021) In The Journal of Organic Chemistry 86(12). p.8248-8262
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.

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author
; ; ; ; ; ; ; ; and
publishing date
type
Contribution to journal
publication status
published
in
The Journal of Organic Chemistry
volume
86
issue
12
pages
15 pages
publisher
The American Chemical Society (ACS)
external identifiers
  • scopus:85108448442
ISSN
1520-6904
DOI
10.1021/acs.joc.1c00707
language
English
LU publication?
no
additional info
Publisher Copyright: © 2021 American Chemical Society.
id
c723c61f-f784-419d-88a5-3640537d8c20
date added to LUP
2025-08-06 19:47:30
date last changed
2025-09-01 11:21:35
@article{c723c61f-f784-419d-88a5-3640537d8c20,
  abstract     = {{<p>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.</p>}},
  author       = {{Clementson, Sebastian and Matheu, Sergio Armentia and Rørsted, Emil Märcher and Pedersen, Henrik and Jensen, Anders A. and Clausen, Rasmus P. and Vital, Paulo and Glibstrup, Emil and Jessing, Mikkel and Kristensen, Jesper L.}},
  issn         = {{1520-6904}},
  language     = {{eng}},
  number       = {{12}},
  pages        = {{8248--8262}},
  publisher    = {{The American Chemical Society (ACS)}},
  series       = {{The Journal of Organic Chemistry}},
  title        = {{Erythrina Alkaloid Analogues as nAChR Antagonists-A Flexible Platform for Leads in Drug Discovery}},
  url          = {{http://dx.doi.org/10.1021/acs.joc.1c00707}},
  doi          = {{10.1021/acs.joc.1c00707}},
  volume       = {{86}},
  year         = {{2021}},
}