Abstract
The functions of melatonin, the hormone of the pineal gland, are of considerable current interest. Synthetic melatonin analogues as agonists and antagonists have been explored in some detail and the molecule can be considered as consisting of an indole core, acting mainly as a spacer, and the 5-methoxyl and 3-amidoethyl side chains acting as the functional components, as originally proposed by Heward and Hadley. This review focuses on the synthetic routes to these melatonin analogues, first of the core, then of the substituents that have been attached to the core, and finally those compounds with restricted conformations and those that are chiral. The importance of the various factors involved in the activity of the compounds as agonist or antagonists is indicated, as is the difference in activity of enantiomers.
Keywords: Benzodioxane, Tetrahydrocarbazoles, restricted conformations, Polycyclic Ring Systems, Oxygenated heterocycles
Mini-Reviews in Medicinal Chemistry
Title: Synthesis of Compounds as Melatonin Agonists and Antagonists
Volume: 7 Issue: 10
Author(s): Peter J. Garratt and Andrew Tsotinis
Affiliation:
Keywords: Benzodioxane, Tetrahydrocarbazoles, restricted conformations, Polycyclic Ring Systems, Oxygenated heterocycles
Abstract: The functions of melatonin, the hormone of the pineal gland, are of considerable current interest. Synthetic melatonin analogues as agonists and antagonists have been explored in some detail and the molecule can be considered as consisting of an indole core, acting mainly as a spacer, and the 5-methoxyl and 3-amidoethyl side chains acting as the functional components, as originally proposed by Heward and Hadley. This review focuses on the synthetic routes to these melatonin analogues, first of the core, then of the substituents that have been attached to the core, and finally those compounds with restricted conformations and those that are chiral. The importance of the various factors involved in the activity of the compounds as agonist or antagonists is indicated, as is the difference in activity of enantiomers.
Export Options
About this article
Cite this article as:
Garratt J. Peter and Tsotinis Andrew, Synthesis of Compounds as Melatonin Agonists and Antagonists, Mini-Reviews in Medicinal Chemistry 2007; 7 (10) . https://dx.doi.org/10.2174/138955707782110132
DOI https://dx.doi.org/10.2174/138955707782110132 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
- 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
Related Articles
-
The Infectious Etiology of Alzheimer’s Disease
Current Neuropharmacology History and Evolution of Reproductive and Developmental Toxicology Guidelines
Current Pharmaceutical Design Novel Approaches in the Treatment of Antipsychotic-Induced Hyperprolactinemia: The Role of Partial Agonists of D2 Dopaminergic Receptors
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Immunomodulatory Roles of VIP and PACAP in Models of Multiple Sclerosis
Current Pharmaceutical Design Prognostic Value of Copeptin in Chronic Kidney Disease: From General Population to End-Stage Renal Disease
Current Protein & Peptide Science Collateral Damage: Contribution of Peripheral Inflammation to Neurodegenerative Diseases
Current Topics in Medicinal Chemistry The Biology of the Sodium Iodide Symporter and its Potential for Targeted Gene Delivery
Current Cancer Drug Targets Fundamental Concepts of the Angiogenic Process
Current Molecular Medicine Protein Kinase C and Prostate Carcinogenesis: Targeting the Cell Cycle and Apoptotic Mechanisms
Current Drug Targets Key Sites for P2X Receptor Function and Multimerization: Overview of Mutagenesis Studies on a Structural Basis
Current Medicinal Chemistry IgG4 Related Syndrome: Another Multiorgan Disease in the Interest Field of Internal Medicine
Current Pharmaceutical Design Therapeutic Approach to Multiple Sclerosis by Novel Oral Drugs
Recent Patents on Inflammation & Allergy Drug Discovery Curcumin, an Active Constiuent of the Ancient Medicinal Herb Curcuma longa L.: Some Uses and the Establishment and Biological Basis of Medical Efficacy
CNS & Neurological Disorders - Drug Targets Pharmacomimetics of Exercise: Novel Approaches for Hippocampally- Targeted Neuroprotective Agents
Current Medicinal Chemistry PET Studies on P-Glycoprotein Function in the Blood-Brain Barrier: How it Affects Uptake and Binding of Drugs within the CNS
Current Pharmaceutical Design Effects of Physical Exercise on Inflammatory Markers of Atherosclerosis
Current Pharmaceutical Design Inhibitors of the Microsomal Prostaglandin E2 Synthase-1 as Alternative to Non Steroidal Anti-Inflammatory Drugs (NSAIDs) – A Critical Review
Current Medicinal Chemistry New Derivatives of GnRH as Potential Anticancer Therapeutic Agents
Current Medicinal Chemistry Occurrence and Severity of Adverse Reactions of Immune Checkpoint Inhibitors (PD-1 and PD L1) Based on Mordovian Dispensary Data Analysis
Current Cancer Therapy Reviews Regulation of Innate Immune Responses in the Central Nervous System
CNS & Neurological Disorders - Drug Targets