Abstract
Choline analogues such as bis-thiazolium salts are thought to inhibit choline transport into Plasmodiuminfected erythrocytes, thus preventing parasite PC biosynthesis, and also to interact with plasmodial haemoglobin degradation in the food vacuole. This new and multiple mode of action is a major asset of these new class of antimalarials, as they could help delay resistance development. We synthesized and designed various sets of analogues, notably prodrugs, since the oral bioavailability of bis-thiazolium salts is relatively low. The chemistry underlying this synthesis relies on inexpensive and readily available starting materials and is straightforward. This is essential since the ultimate objective is to obtain affordable and orally available drugs for uncomplicated malaria treatment.
Keywords: Antimalarials, choline analogues, phospholipid, plasmodium, prodrugs, thiazolium salts.
Current Topics in Medicinal Chemistry
Title:Exploring Prodrug Approaches for Albitiazolium and its Analogues
Volume: 14 Issue: 14
Author(s): Suzanne Peyrottes, Sergio Caldarelli, Sharon Wein, Christian Perigaud and Henri Vial
Affiliation:
Keywords: Antimalarials, choline analogues, phospholipid, plasmodium, prodrugs, thiazolium salts.
Abstract: Choline analogues such as bis-thiazolium salts are thought to inhibit choline transport into Plasmodiuminfected erythrocytes, thus preventing parasite PC biosynthesis, and also to interact with plasmodial haemoglobin degradation in the food vacuole. This new and multiple mode of action is a major asset of these new class of antimalarials, as they could help delay resistance development. We synthesized and designed various sets of analogues, notably prodrugs, since the oral bioavailability of bis-thiazolium salts is relatively low. The chemistry underlying this synthesis relies on inexpensive and readily available starting materials and is straightforward. This is essential since the ultimate objective is to obtain affordable and orally available drugs for uncomplicated malaria treatment.
Export Options
About this article
Cite this article as:
Peyrottes Suzanne, Caldarelli Sergio, Wein Sharon, Perigaud Christian and Vial Henri, Exploring Prodrug Approaches for Albitiazolium and its Analogues, Current Topics in Medicinal Chemistry 2014; 14 (14) . https://dx.doi.org/10.2174/1568026614666140808121746
DOI https://dx.doi.org/10.2174/1568026614666140808121746 |
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
-
The Linkage “Body Mass Index-Insomnia Levels-Eating Disorder Flexibility”
in Italian Nurses During the Covid-19 Outbreak: A Psychoendocrinological
Employment Disease
Endocrine, Metabolic & Immune Disorders - Drug Targets COVID-19 and Type 2 Diabetes Mellitus: HCQ may be the Holy Grail
Infectious Disorders - Drug Targets Molecular Modeling and Dynamics Simulation Analysis of KATNAL1 for Identification of Novel Inhibitor of Sperm Maturation
Combinatorial Chemistry & High Throughput Screening From Dual Binding Site Acetylcholinesterase Inhibitors to Multi-Target-Directed Ligands (MTDLs): A Step Forward in the Treatment of Alzheimers Disease
Mini-Reviews in Medicinal Chemistry Naturally Occurring and Synthetic Imidazoles: Their Chemistry and Their Biological Activities
Current Medicinal Chemistry The Use of Infliximab in Dermatology
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Review of the Essential Oil Composition of Iranian Endemic and Native Taxa of Apiaceae (Umbelliferae)
Current Organic Chemistry The CXCL12/CXCR4 Axis as a Therapeutic Target in Cancer and HIV-1 Infection
Current Medicinal Chemistry Discovery and Development of Cyclin-Dependent Kinase 8 Inhibitors
Current Medicinal Chemistry Preface
Current Enzyme Inhibition Some Ways for the Synthesis of Chalcones - New Ways for the Synthesis of Flavon-3-ols
Mini-Reviews in Organic Chemistry Design, Synthesis and Antimycobacterial Activity of Some New Azaheterocycles: Phenanthroline with p-halo-benzoyl Skeleton. Part V
Letters in Drug Design & Discovery Acronycine Derivatives: A Promising Series of Anti-Cancer Agents
Anti-Cancer Agents in Medicinal Chemistry New Developments in the Discovery of Agents to Treat Hepatitis C
Current Topics in Medicinal Chemistry Diagnosis and Possible Use of Traditional Medicinal Plant to combat COVID-19
Coronaviruses A2A Receptor Ligands: Past, Present and Future Trends
Current Topics in Medicinal Chemistry G-quadruplex DNA Aptamers and their Ligands: Structure, Function and Application
Current Pharmaceutical Design Contextualizing the Genes Altered in Bladder Neoplasms in Pediatric and Teen Patients Allows Identifying Two Main Classes of Biological Processes Involved and New Potential Therapeutic Targets
Current Genomics Experimental and Theoretical Advances in Functional Understanding of Flavonoids as Anti-Tumor Agents
Anti-Cancer Agents in Medicinal Chemistry Combination Therapy with Favipiravir for Treatment of Hospitalized COVID-19 Adults
New Emirates Medical Journal