Abstract
The extraordinary pharmacology of nicotine and epibatidine have indicated the potential for nicotinic acetylcholine receptor (nAChR) ligands to serve as a new therapeutic class for a host of CNS disorders. Many such ligands are natural products, or analogs thereof, which represent a significant challenge to the synthetic chemist. Synthesis of such molecules often serves as a showcase to demonstrate the potential of newly developed methodology. This synthetic challenge coupled with the promise of pharmacological activity in compounds possessing the nicotinic pharmacophore has stimulated a great deal of synthetic activity over the last five years. The present report provides an overview of novel synthetic methodology occurring during this period directed toward the synthesis of compounds with presumed affinity for the neuronal nAChR. Syntheses chosen for review here represent the major efforts toward molecules such as epibatidine analogs, anatoxin-a, nicotine and related alkaloids, conformationally constrained nicotine derivatives, cytisine and methyllycaconitine (MLA).
Keywords: Nicotinic Acetylcholine Receptor, pharmacophore, neuronal nAChR, alkaloids, methyllycaconitine (MLA)
Current Topics in Medicinal Chemistry
Title: Recent Developments in the Synthesis of Nicotinic Acetylcholine Receptor Ligands
Volume: 4 Issue: 6
Author(s): Scott R. Breining
Affiliation:
Keywords: Nicotinic Acetylcholine Receptor, pharmacophore, neuronal nAChR, alkaloids, methyllycaconitine (MLA)
Abstract: The extraordinary pharmacology of nicotine and epibatidine have indicated the potential for nicotinic acetylcholine receptor (nAChR) ligands to serve as a new therapeutic class for a host of CNS disorders. Many such ligands are natural products, or analogs thereof, which represent a significant challenge to the synthetic chemist. Synthesis of such molecules often serves as a showcase to demonstrate the potential of newly developed methodology. This synthetic challenge coupled with the promise of pharmacological activity in compounds possessing the nicotinic pharmacophore has stimulated a great deal of synthetic activity over the last five years. The present report provides an overview of novel synthetic methodology occurring during this period directed toward the synthesis of compounds with presumed affinity for the neuronal nAChR. Syntheses chosen for review here represent the major efforts toward molecules such as epibatidine analogs, anatoxin-a, nicotine and related alkaloids, conformationally constrained nicotine derivatives, cytisine and methyllycaconitine (MLA).
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Cite this article as:
Breining R. Scott, Recent Developments in the Synthesis of Nicotinic Acetylcholine Receptor Ligands, Current Topics in Medicinal Chemistry 2004; 4 (6) . https://dx.doi.org/10.2174/1568026043451131
DOI https://dx.doi.org/10.2174/1568026043451131 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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