Abstract
Chagas disease is the major endemic disease in South and Central America caused by a trypanosomatid parasite (Trypanosoma cruzi). The current treatment relies on two old and nonspecific chemotherapeutic agents, Nifurtimox and Benznidazole. Despite the major advances that have been made in the identification of specific targets that afford selectivity, the drugs used today have serious side effects. Furthermore, differences in drug susceptibility among different T. cruzi isolates have led to varied parasitological cure rates depending on the geographical region. There is, therefore, an urgent need for the development of new antichagasic drugs. In this regard we have spent more than a decade in the search for more effective agents able to compromise the proliferation of T. cruzi. We began our research with our own compounds and then continued with compounds from other researcher groups. We systematically characterized representatives of a wide range of different chemical families. In this review we summarize our ongoing efforts to identify potential anti-T. cruzi agents using our compound-library. It is discussed and presented the structure- activity relationship observed among the different groups of chemical families.
Keywords: Chagas' disease, Trypanosoma cruzi, antichagasic drugs, Nifurtimox, Benznidazole, chemotherapeutic agents
Mini-Reviews in Medicinal Chemistry
Title: Anti-T. cruzi Agents: Our Experience in the Evaluation of More than Five Hundred Compounds
Volume: 8 Issue: 13
Author(s): Hugo Cerecetto and Mercedes Gonzalez
Affiliation:
Keywords: Chagas' disease, Trypanosoma cruzi, antichagasic drugs, Nifurtimox, Benznidazole, chemotherapeutic agents
Abstract: Chagas disease is the major endemic disease in South and Central America caused by a trypanosomatid parasite (Trypanosoma cruzi). The current treatment relies on two old and nonspecific chemotherapeutic agents, Nifurtimox and Benznidazole. Despite the major advances that have been made in the identification of specific targets that afford selectivity, the drugs used today have serious side effects. Furthermore, differences in drug susceptibility among different T. cruzi isolates have led to varied parasitological cure rates depending on the geographical region. There is, therefore, an urgent need for the development of new antichagasic drugs. In this regard we have spent more than a decade in the search for more effective agents able to compromise the proliferation of T. cruzi. We began our research with our own compounds and then continued with compounds from other researcher groups. We systematically characterized representatives of a wide range of different chemical families. In this review we summarize our ongoing efforts to identify potential anti-T. cruzi agents using our compound-library. It is discussed and presented the structure- activity relationship observed among the different groups of chemical families.
Export Options
About this article
Cite this article as:
Cerecetto Hugo and Gonzalez Mercedes, Anti-T. cruzi Agents: Our Experience in the Evaluation of More than Five Hundred Compounds, Mini-Reviews in Medicinal Chemistry 2008; 8 (13) . https://dx.doi.org/10.2174/138955708786369528
DOI https://dx.doi.org/10.2174/138955708786369528 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Drugs and mitochondria
Mitochondria play a central role in the life and death of cells. They are not merely the center for energy metabolism but are also the headquarters for different catabolic and anabolic processes, calcium fluxes, and various signaling pathways. Mitochondria maintain homeostasis in the cell by interacting with reactive oxygen-nitrogen species ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer’s, Parkinson’s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
Related Articles
-
Gemcitabine-Related Atrial Fibrillation: A Case Report and Review of the
Literature
Current Drug Safety Remediation of Cellular Hypoxic Damage by Pharmacological Agents
Current Pharmaceutical Design Inflamm-ageing and senescence in gout: the tale of an old king’s disease.
Current Aging Science Disruption of Circadian Rhythms and Sleep on Critical Illness and the Impact on Cardiovascular Events
Current Pharmaceutical Design Preface
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Simultaneous Determination of Saponins and Lignans in Rat Plasma by UPLC- MS/MS and its Application to a Pharmacokinetic Study of Shenqi Jiangtang Granule
Current Drug Metabolism Diabetes and Chronic Heart Failure: From Diabetic Cardiomyopathy to Therapeutic Approach
Endocrine, Metabolic & Immune Disorders - Drug Targets Role of Vitamins in Cardiovascular Health: Know Your Facts-Part 2
Current Vascular Pharmacology Rac-1 as a New Therapeutic Target in Cerebro- and Cardio-Vascular Diseases
Current Drug Targets Omecamtiv Mecarbil: A Myosin Motor Activator Agent with Promising Clinical Performance and New in vitro Results
Current Medicinal Chemistry Common Genetic Conditions of Ischemic Stroke to Keep in Mind
Current Molecular Medicine Effects of Sodium-Glucose Cotransporter-2 Inhibitors on Cardiac Structural and Electrical Remodeling: From Myocardial Cytology to Cardiodiabetology
Current Vascular Pharmacology Key miRNAs in Modulating Aging and Longevity: A Focus on Signaling Pathways and Cellular Targets
Current Molecular Pharmacology Cardio-Protective Effects of Sodium-Glucose Co-Transporter 2 Inhibitors: Focus on Heart Failure
Current Pharmaceutical Design Effects of Acute and Chronic Biomechanical Strain on Human Cerebral Endothelial Cells in Altering their Proteome Profile
Current Proteomics Adult Stem Cell Therapy for Cardiac Repair in Patients After Acute Myocardial Infarction Leading to Ischemic Heart Failure: An Overview of Evidence from the Recent Clinical Trials
Current Cardiology Reviews LCHAD and MTP Deficiencies - Two Disorders of Mitochondrial Fatty Acid β-Oxidation with Unusual Features
Current Pediatric Reviews The Role of Chemokines, Cytokines and Adhesion Molecules in Stem Cell Trafficking and Homing
Current Pharmaceutical Design Pharmacogenetics of Target Genes Across Doxorubicin Disposition Pathway: A Review
Current Drug Metabolism HER2 in the Era of Molecular Medicine: A Review
Current Cancer Therapy Reviews