Abstract
Of the tropical diseases, trypanosomiases and leishmaniases should most concern the pharmaceutical community because of their high prevalence in developing countries and the lack of effective drug treatments. Despite this, they have not historically received much attention in terms of investment and research effort, nor do they now. In very recent years, thanks to the involvement of several nonprofit organizations, the chemotherapeutic options have expanded with the introduction of the first combination therapy. The optimal efficacy and safety of nifurtimox – eflornithine combination against second-stage human African trypanosomiasis is an encouraging first step towards simpler and more affordable therapies. Along the same line, I propose that single chemical entities able to modulate more than one target may prove more efficacious and tolerable than the available arsenal of drugs. Herein, I discuss the pros and cons of this approach, together with examples taken from the recent literature.
Keywords: Neglected tropical diseases, combination therapy, multitarget drug discovery, hybrid compounds, leishmaniasis, trypanosomiasis, multitarget ligands, Nifurtimox benznidazole, toxic organic compound, mucocutaneous disease, chronic human trypanosomiasis, therapeutic compounds, antiretroviral treatment, visceralleishmaniases, axenic amastigote
Current Topics in Medicinal Chemistry
Title: Multi-Target-Directed Ligands as Innovative Tools to Combat Trypanosomatid Diseases
Volume: 11 Issue: 22
Author(s): Maria Laura Bolognesi
Affiliation:
Keywords: Neglected tropical diseases, combination therapy, multitarget drug discovery, hybrid compounds, leishmaniasis, trypanosomiasis, multitarget ligands, Nifurtimox benznidazole, toxic organic compound, mucocutaneous disease, chronic human trypanosomiasis, therapeutic compounds, antiretroviral treatment, visceralleishmaniases, axenic amastigote
Abstract: Of the tropical diseases, trypanosomiases and leishmaniases should most concern the pharmaceutical community because of their high prevalence in developing countries and the lack of effective drug treatments. Despite this, they have not historically received much attention in terms of investment and research effort, nor do they now. In very recent years, thanks to the involvement of several nonprofit organizations, the chemotherapeutic options have expanded with the introduction of the first combination therapy. The optimal efficacy and safety of nifurtimox – eflornithine combination against second-stage human African trypanosomiasis is an encouraging first step towards simpler and more affordable therapies. Along the same line, I propose that single chemical entities able to modulate more than one target may prove more efficacious and tolerable than the available arsenal of drugs. Herein, I discuss the pros and cons of this approach, together with examples taken from the recent literature.
Export Options
About this article
Cite this article as:
Laura Bolognesi Maria, Multi-Target-Directed Ligands as Innovative Tools to Combat Trypanosomatid Diseases, Current Topics in Medicinal Chemistry 2011; 11 (22) . https://dx.doi.org/10.2174/156802611798184391
DOI https://dx.doi.org/10.2174/156802611798184391 |
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
-
Subpopulations of Bone Marrow Mesenchymal Stem Cells Exhibit Differential Effects in Delaying Retinal Degeneration
Current Molecular Medicine Early Prediction of Preeclampsia: Hope for Early Intervention?
Current Women`s Health Reviews Nitric Oxide Modulation as a Potential Molecular Mechanism Underlying the Protective Role of NaHS in Liver Ischemia Reperfusion Injury
Current Molecular Pharmacology Acetylome Regulation by Sirtuins in the Brain: From Normal Physiology to Aging and Pathology
Current Pharmaceutical Design Use of Medication in Coronary Imaging by CT
Current Medical Imaging In Vitro CYP2D Inhibitory Effect and Influence on Pharmacokinetics and Pharmacodynamic Parameters of Metoprolol Succinate by Terminalia arjuna in Rats
Drug Metabolism Letters Screening for Inhibitors of Microglia to Reduce Neuroinflammation
CNS & Neurological Disorders - Drug Targets Aliskiren, a Direct Renin Inhibitor, in Clinical Practice: A New Approach in the Treatment of Hypertension
Current Vascular Pharmacology Anacetrapib: A New Weapon Against Dyslipidemia
Current Clinical Pharmacology Nano-Delivery in Pediatric Tumors: Looking Back, Moving Forward
Anti-Cancer Agents in Medicinal Chemistry [177Lu]-DOTA0-Tyr3-Octreotate: A Potential Targeted Radiotherapeutic for the Treatment of Medulloblastoma
Current Radiopharmaceuticals STABIL-study: The Course of Therapy, Safety and Pharmacokinetic Parameters of Conversion of Prograf® to Tacrolimus HEXAL®/Crilomus® in Renal Transplant Recipients – an Observational Study in Germany
Current Reviews in Clinical and Experimental Pharmacology Cigarette Smoke-Induced Proteostasis Imbalance in Obstructive Lung Diseases
Current Molecular Medicine Metformin and Anti-Cancer Therapeutics: Hopes for a More Enhanced Armamentarium Against Human Neoplasias?
Current Medicinal Chemistry Pyrazolo[4,3-e][1,2,4]Triazolo[1,5-c]Pyrimidine Template: Organic and Medicinal Chemistry Approach
Current Organic Chemistry Cardiac and Pulmonary Manifestations in the Antiphospholipid Syndrome
Current Rheumatology Reviews Age-related Changes in Respiratory Function and Daily Living. A Tentative Model Including Psychosocial Variables, Respiratory Diseases and Cognition
Current Aging Science Novel Possible Pharmaceutical Research Tools: Stem Cells, Gene Delivery and their Combination
Current Pharmaceutical Design G Protein-Coupled Receptor Signaling Complexity in Neuronal Tissue:Implications for Novel Therapeutics
Current Alzheimer Research Antipsychotic Use and Mortality Risk in Community-Dwelling Alzheimer’s Disease Patients: Evidence for a Role of Dementia Severity
Current Alzheimer Research