Erythrina Alkaloid Analogues as nAChR Antagonists-A Flexible Platform for Leads in Drug Discovery
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Erythrina Alkaloid Analogues as nAChR Antagonists-A Flexible Platform for Leads in Drug Discovery. / Clementson, Sebastian; Matheu, Sergio Armentia; Rørsted, Emil Märcher; Pedersen, Henrik; Jensen, Anders A; Clausen, Rasmus P; Vital, Paulo; Glibstrup, Emil; Jessing, Mikkel; Kristensen, Jesper L.
I: The Journal of Organic Chemistry, Bind 86, Nr. 12, 2021, s. 8248-8262.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Erythrina Alkaloid Analogues as nAChR Antagonists-A Flexible Platform for Leads in Drug Discovery
AU - Clementson, Sebastian
AU - Matheu, Sergio Armentia
AU - Rørsted, Emil Märcher
AU - Pedersen, Henrik
AU - Jensen, Anders A
AU - Clausen, Rasmus P
AU - Vital, Paulo
AU - Glibstrup, Emil
AU - Jessing, Mikkel
AU - Kristensen, Jesper L
PY - 2021
Y1 - 2021
N2 - 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.
AB - 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.
U2 - 10.1021/acs.joc.1c00707
DO - 10.1021/acs.joc.1c00707
M3 - Journal article
C2 - 34061521
VL - 86
SP - 8248
EP - 8262
JO - Journal of Organic Chemistry
JF - Journal of Organic Chemistry
SN - 0022-3263
IS - 12
ER -
ID: 270553746