Nitroheterocyclic derivatives: privileged scaffold for drug development against Chagas disease

AbstractChagas disease or American trypanosomiasis is a major public health problem in Latin America. Approximately seven million people are currently infected worldwide. Despite the efforts to develop new drugs, only two nitroheterocyclic drugs (nifurtimox and benznidazole) are available for the treatment of Chagas disease, These drugs have been available since the 1970s, and no new drugs have been approved. Due to the lack of alternatives for the treatment of this disease, this review describes recent advances (2013 –2019) concerning nitroheterocyclic compounds with activity againstT. cruzi parasites, as well as new perspectives for future research.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research

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Publication date: Available online 3 December 2019Source: Journal of Molecular Graphics and ModellingAuthor(s): Edward A. Valera-Vera, Melisa Sayé, Chantal Reigada, Mariana R. Miranda, Claudio A. PereiraAbstractEnolase is a glycolytic enzyme that catalyzes the interconversion between 2-phosphoglycerate and phosphoenolpyruvate. In trypanosomatids, enolase was proposed as a key enzyme after in silico and in vivo analysis and it was validated as a protein essential for the survival of the parasite. Therefore, enolase constitutes an interesting enzyme target for the identification of drugs against Chagas disease. In thi...
Source: Journal of Molecular Graphics and Modelling - Category: Molecular Biology Source Type: research
CONCLUSIONS: Chagas disease affected mostly women, with the indeterminate chronic form of the disease.
Source: Revista da Sociedade Brasileira de Medicina Tropical - Category: Tropical Medicine Source Type: research
In the Yucat án Peninsula, Mexico, Triatoma dimidiata is the main vector of Trypanosoma cruzi, the causative agent of Chagas disease. Little effort has been made to identify blood meal sources of T. dimidiata in n...
Source: Parasites and Vectors - Category: Microbiology Authors: Tags: Research Source Type: research
A question of epidemiological relevance in Chagas disease studies is to understand Trypanosoma cruzi transmission cycles and trace the origins of (re)emerging cases in areas under vector or disease surveillance. ...
Source: Parasites and Vectors - Category: Microbiology Authors: Tags: Methodology Source Type: research
Trypanosoma cruzi infection causes Chagas disease, which affects 7 million people worldwide. Two drugs are available to treat it: benznidazole and nifurtimox. Although both are efficacious against the acute stage of the disease, this is usually asymptomatic and goes undiagnosed and untreated. Diagnosis is achieved at the chronic stage, when life-threatening heart and/or gut tissue disruptions occur in ~30% of those chronically infected. By then, the drugs' efficacy is reduced, but not their associated high toxicity. Given current deficiencies in diagnosis and treatment, a vaccine to prevent infection and/or the development...
Source: Frontiers in Immunology - Category: Allergy & Immunology Source Type: research
CONCLUSIONS: These data contribute to a better understanding of the distribution of T. cruzi infection in the Northeastern region of Brazil. Preventive measures based on vector control should be implemented in the study ar ea in order to reduce the burden this neglected tropical disease.
Source: Revista da Sociedade Brasileira de Medicina Tropical - Category: Tropical Medicine Source Type: research
Publication date: Available online 12 November 2019Source: MicronAuthor(s): Andrezza Raposo Borges de Melo, Taciana Mirely Maciel Higino, Aline Dulce Pitt da Rocha Oliveira, Adriana Fontes, Diego César Nunes da Silva, Maria Carolina Accioly Brelaz de Castro, José Arimatéia Dantas Lopes, Regina Celia Bressan Queiroz de FigueiredoAbstractChagas disease, caused by the protozoan Trypanosoma cruzi, is considered a public health problem. The current chemotherapy for this illness causes serious side effects and its use in the chronic phase of the disease is still controversial. In this sense, the investigatio...
Source: Micron - Category: Biology Source Type: research
Trypanosoma cruzi is the causative agent of Chagas disease, which is endemic to subtropical and tropical Americas. The disease treatment remains partially ineffective, involving therapies directed to the parasite...
Source: Parasites and Vectors - Category: Microbiology Authors: Tags: Research Source Type: research
Abstract Chagas disease (CD), caused by Trypanosoma cruzi, is the main parasitic disease in the Western Hemisphere, with an increasing number of cases, especially in non-endemic regions. The disease is characterized by cardiomegaly and mega viscera, nevertheless, the clinical outcome is hard to predict, underscoring the need for further research into the pathophysiology of CD. Even though most basic and translational research involving CD is performed using in vivo models, in vitro models arise as an ethical, rapidly evolving, and physiologically relevant alternative for CD research. In the present review, we disc...
Source: Acta Tropica - Category: Infectious Diseases Authors: Tags: Acta Trop Source Type: research
jo JA, Ferreira A Abstract Microbes have developed mechanisms to resist the host immune defenses and some elicit antitumor immune responses. About 6 million people are infected with Trypanosoma cruzi, the protozoan agent of Chagas' disease, the sixth neglected tropical disease worldwide. Eighty years ago, G. Roskin and N. Klyuyeva proposed that T. cruzi infection mediates an anti-cancer activity. This observation has been reproduced by several other laboratories, but no molecular basis has been proposed. We have shown that the highly pleiotropic chaperone calreticulin (TcCalr, formerly known as TcCRT), translocate...
Source: Immunobiology - Category: Allergy & Immunology Authors: Tags: Immunobiology Source Type: research
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