Design, synthesis, and biological evaluation of erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists

…, M Borch, JT Andreasen, J Andersen…

Index: Crestey, Francois; Jensen, Anders A.; Borch, Morten; Andreasen, Jesper Tobias; Andersen, Jacob; Balle, Thomas; Kristensen, Jesper Langgaard Journal of Medicinal Chemistry, 2013 , vol. 56, # 23 p. 9673 - 9682

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Citation Number: 12

Abstract

The synthesis of a new series of Erythrina alkaloid analogues and their pharmacological characterization at various nicotine acetylcholine receptor (nAChR) subtypes are described. The compounds were designed to be simplified analogues of aromatic erythrinanes with the aim of obtaining subtype-selective antagonists for the nAChRs and thereby probe the potential of using these natural products as scaffolds for further ligand optimization. The ...