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
-
Fe3O4 Nanoparticles Mediated Synthesis of Novel Isatin-dihydropyrimidinone Hybrid Molecules as Antioxidant and Cytotoxic Agents
Anti-Cancer Agents in Medicinal Chemistry Lead Compounds for Anti-inflammatory Drugs Isolated from the Plants of the Traditional Oriental Medicine in Korea
Inflammation & Allergy - Drug Targets (Discontinued) A Pathogenetic Approach to Autoimmune Skin Disease Therapy: Psoriasis and Biological Drugs, Unresolved Issues, and Future Directions
Current Pharmaceutical Design Pathophysiology of Idiopathic Atrial Fibrillation - Prognostic and Treatment Implications
Current Pharmaceutical Design Synergistic Antiproliferative and Antiangiogenic Effects of EGFR and mTOR Inhibitors
Current Pharmaceutical Design The Guinea Pig as an Animal Model for Asthma
Current Drug Targets Atopic Dermatitis in the Elderly
Inflammation & Allergy - Drug Targets (Discontinued) An Update on Natural Products with Carbonic Anhydrase Inhibitory Activity
Current Pharmaceutical Design Structure-based Design of Mimetics for Granulocyte-macrophage Colony Stimulating Factor (GM-CSF)
Current Pharmaceutical Design Dyslipidemia as a Risk Factor for Ischemic Stroke
Current Topics in Medicinal Chemistry Promising Protective Effects of Chrysin in Cardiometabolic Diseases
Current Drug Targets Potential Benefits of Glitazones for Cancer and Vascular Disease
Current Drug Therapy New Pharmacological Approaches to the Cholinergic System: An Overview on Muscarinic Receptor Ligands and Cholinesterase Inhibitors
Recent Patents on CNS Drug Discovery (Discontinued) Current Status and Future Prospects of C1 Domain Ligands as Drug Candidates
Current Topics in Medicinal Chemistry Cardioprotective Effects of the Polyphenol Hydroxytyrosol from Olive Oil
Current Drug Targets The Cardiovascular Protective Effects of Chrysin: A Narrative Review on Experimental Researches
Cardiovascular & Hematological Agents in Medicinal Chemistry New Insights for Multifactorial Disease Therapy: The Challenge of the Symbiotic Drugs
Current Drug Therapy Beyond Bile Acids: Targeting Farnesoid X Receptor (FXR) with Natural and Synthetic Ligands
Current Topics in Medicinal Chemistry Imaging Agents in Targeting Tumor Hypoxia
Current Medicinal Chemistry Drug Delivery Systems Based on Titania Nanotubes and Active Agents for Enhanced Osseointegration of Bone Implants
Current Medicinal Chemistry