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).
Export Options
About this article
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 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Tyrosine Kinase Update: Role and Response in Cancer Therapy
Current Cancer Therapy Reviews Patent Selections:
Recent Patents on Cardiovascular Drug Discovery Can Dietary Polyphenols Prevent the Formation of Toxic Compounds from Maillard Reaction?
Current Drug Metabolism Beneficiary and Adverse Effects of Phytoestrogens: A Potential Constituent of Plant-based Diet
Current Pharmaceutical Design Patent Selections
Recent Patents on CNS Drug Discovery (Discontinued) Cysteinyl Leukotriene Receptor Antagonists and Thromboxane Synthase Inhibitors: New Targets to Treat Asthma
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Inhibitors and Breakers of Advanced Glycation Endproducts (AGEs): A Review
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Targeted Therapies in Non-Small Cell Lung Cancer: Proven Concepts and Unfulfilled Promises.
Current Cancer Drug Targets Interaction of Nerve Agent Antidotes with Cholinergic Systems
Current Medicinal Chemistry Monoclonal Antibodies as Cancer Therapeutics
Recent Patents on Biotechnology Application of RNA Interference for the Control of Female Reproductive Functions
Current Pharmaceutical Design The Complex Inter-Relationship Between Diabetes and Schizophrenia
Current Diabetes Reviews Using Extracellular Matrix-Derived Peptides to Alter the Microenvironment for Myocardial Repair
Current Vascular Pharmacology ESVS Guidelines: Section B - Diagnosis and Investigation of Patients with Carotid Stenosis
Current Vascular Pharmacology The cAMP-Dependent Protein Kinase Pathway as Therapeutic Target – Possibilities and Pitfalls
Current Topics in Medicinal Chemistry Rho Kinase Inhibitors and Novel Ocular Drug Delivery Systems- A Revolutionary Step Towards the Treatment of Glaucoma
Current Drug Delivery Natural Therapies of the Inflammatory Bowel Disease: The Case of Rutin and its Aglycone, Quercetin
Mini-Reviews in Medicinal Chemistry Recent Progress in the Development of Agonists and Antagonists for Melatonin Receptors
Current Medicinal Chemistry Epidemiology and Clinical Presentation of Stress-Related Peptic Damage and Chronic Peptic Ulcer
Current Molecular Medicine Inhibition of Matrix Metalloproteinases as a Feasible Therapeutic Target in Rheumatoid Arthritis
Current Rheumatology Reviews