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https://www.readbyqxmd.com/read/29031078/structural-design-synthesis-and-pharmacological-evaluation-of-thiazoles-against-trypanosoma-cruzi
#1
Gevanio Bezerra de Oliveira Filho, Marcos Veríssimo de Oliveira Cardoso, José Wanderlan Pontes Espíndola, Dayane Albuquerque Oliveira E Silva, Rafaela Salgado Ferreira, Pollyanne Lacerda Coelho, Pâmela Silva Dos Anjos, Emanuelle de Souza Santos, Cássio Santana Meira, Diogo Rodrigo Magalhaes Moreira, Milena Botelho Pereira Soares, Ana Cristina Lima Leite
Chagas disease is one of the most significant health problems in the American continent. benznidazole (BDZ) and nifurtimox (NFX) are the only drugs approved for treatment and exhibit strong side effects and ineffectiveness in the chronic stage, besides different susceptibility among T. cruzi DTUs (Discrete Typing Units). Therefore, new drugs to treat this disease are necessary. Thiazole compounds have been described as potent trypanocidal agents. Here we report the structural planning, synthesis and anti-T...
September 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29016289/experimental-and-clinical-treatment-of-chagas-disease-a-review
#2
Policarpo Ademar Sales Junior, Israel Molina, Silvane Maria Fonseca Murta, Adrián Sánchez-Montalvá, Fernando Salvador, Rodrigo Correa de Oliveira, Cláudia Martins Carneiro
Chagas disease (CD) is caused by the protozoan parasite Trypanosoma cruzi that infects a broad range of triatomines and mammalian species, including man. It afflicts 8 million people in Latin America, and its incidence is increasing in nonendemic countries owing to rising international immigration and nonvectorial transmission routes such as blood donation. Since the 1960s, the only drugs available for the clinical treatment of this infection have been benznidazole and nifurtimox (NFX). Treatment with these trypanocidal drugs is recommended in both the acute and chronic phases of CD...
October 2, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28989779/prostaglandin-f2%C3%AE-synthase-in-trypanosoma-cruzi-plays-critical-roles-in-oxidative-stress-and-susceptibility-to-benznidazole
#3
Paola García-Huertas, Ana María Mejía-Jaramillo, Carlos Renato Machado, Anna Cláudia Guimarães, Omar Triana-Chávez
Nifurtimox (Nfx) and benznidazole (Bz) are the current drugs used for the treatment of Chagas disease. The mechanisms of action and resistance to these drugs in this parasite are poorly known. Prostaglandin F2α synthase or old yellow enzyme (OYE), an NAD(P)H flavin oxidoreductase, has been involved in the activation pathway of other trypanocidal drugs such as Nfx; however, its role in the mechanism of action of Bz is uncertain. In this paper, we performed some experiments of functional genomics in the parasite Trypanosoma cruzi with the aim to test the role of this gene in the resistance to Bz...
September 2017: Royal Society Open Science
https://www.readbyqxmd.com/read/28973960/characterization-and-trypanocidal-activity-of-a-novel-pyranaphthoquinone
#4
Elen Diana Dantas, Fabia Julliana Jorge de Souza, William Nascimento Litaiff Nogueira, Cláudia Cândida Silva, Pedro Henrique Antunes de Azevedo, Cícero Flávio Soares Aragão, Patricia Danielle Oliveira de Almeida, Mariana Filomena do Carmo Cardoso, Fernando de Carvalho da Silva, Eduardo Pereira de Azevedo, Euzébio Guimarães Barbosa, Emerson Silva Lima, Vitor Francisco Ferreira, Ádley Antonini Neves de Lima
Chagas disease is an endemic parasitic infection that occurs in 21 Latin American countries. New therapies for this disease are urgently needed, as the only two drugs available (nifurtimox and benznidazol) have high toxicity and variable efficacy in the disease's chronic phase. Recently, a new chemical entity (NCE) named Pyranaphthoquinone (IVS320) was synthesized from lawsone. We report herein, a detailed study of the physicochemical properties and in vitro trypanocidal activity of IVS320. A series of assays were performed for characterization, where thermal, diffractometric, and morphological analysis were performed...
September 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28941731/trypanosoma-cruzi-genetic-diversity-something-new-for-something-known-about-chagas-disease-manifestations-serodiagnosis-and-drug-sensitivity
#5
REVIEW
Bianca Zingales
The genetic diversity of Trypanosoma cruzi, the protozoan agent of Chagas disease, is widely recognized. At present, T. cruzi is partitioned into seven discrete typing units (DTUs), TcI-TcVI and Tcbat. This article reviews the present knowledge on the parasite population structure, the evolutionary relationships among DTUs and their distinct, but not exclusive ecological and epidemiological associations. Different models for the origin of hybrid DTUs are examined, which agree that genetic exchange among T. cruzi populations is frequent and has contributed to the present parasite population structure...
September 20, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28935948/novel-scaffolds-for-inhibition-of-cruzipain-identified-from-high-throughput-screening-of-anti-kinetoplastid-chemical-boxes
#6
Emir Salas-Sarduy, Lionel Urán Landaburu, Joel X Karpiak, Kevin P Madauss, Juan José Cazzulo, Fernán Agüero, Vanina Eder Alvarez
American Trypanosomiasis or Chagas disease is a prevalent, neglected and serious debilitating illness caused by the kinetoplastid protozoan parasite Trypanosoma cruzi. The current chemotherapy is limited only to nifurtimox and benznidazole, two drugs that have poor efficacy in the chronic phase and are rather toxic. In this scenario, more efficacious and safer drugs, preferentially acting through a different mechanism of action and directed against novel targets, are particularly welcome. Cruzipain, the main papain-like cysteine peptidase of T...
September 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28910299/access-to-benznidazole-for-chagas-disease-in-the-united-states-cautious-optimism
#7
Jonathan D Alpern, Rogelio Lopez-Velez, William M Stauffer
Drugs for neglected tropical diseases (NTD) are being excessively priced in the United States. Benznidazole, the first-line drug for Chagas disease, may become approved by the Food and Drug Administration (FDA) and manufactured by a private company in the US, thus placing it at risk of similar pricing. Chagas disease is an NTD caused by Trypanosoma cruzi; it is endemic to Latin America, infecting 8 million individuals. Human migration has changed the epidemiology causing nonendemic countries to face increased challenges in diagnosing and managing patients with Chagas disease...
September 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28902285/dipyridamole-potentiated-the-trypanocidal-effect-of-nifurtimox-and-improved-the-cardiac-function-in-nmri-mice-with-acute-chagasic-myocarditis
#8
Sonia Santeliz, Peter Caicedo, Elidiosmar Giraldo, Carmen Alvarez, María-Daniela Yustiz, Claudina Rodríguez-Bonfante, Romina Bonfante-Rodríguez, Rafael Bonfante-Cabarcas
BACKGROUND: As chronic Chagas disease does not have a definitive treatment, the development of alternative therapeutic protocols is a priority. Dipyridamole (DPY) is an alternative to counteract the pathophysiological phenomena involved in Chagas cardiomyopathy. OBJECTIVE: To evaluate the therapeutic efficacy of DPY associated with nifurtimox (Nfx) in epimastigote axenic cultures and in mice with acute Chagas disease. METHODS: NMRI adult male mice were divided into nine groups: three healthy and six Trypanosoma cruzi-infected groups...
September 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28870526/drug-repurposing-strategy-against-trypanosoma-cruzi-infection-in-vitro-and-in-vivo-assessment-of-the-activity-of-metronidazole-in-mono-and-combined-therapy
#9
M R Simões-Silva, J S De Araújo, G M Oliveira, K C Demarque, R B Peres, I D'Almeida-Melo, D G J Batista, C F Da Silva, C Cardoso-Santos, P B Da Silva, M M Batista, M T Bahia, M N C Soeiro
Metronidazole (Mtz) is a commercial broad-spectrum nitroimidazolic derivative with relevant antimicrobial activity and relative safety profile. Therefore, it is fair to consider Mtz a candidate for drug repurposing for other neglected conditions such as Chagas disease (CD), a parasitic pathology caused by Trypanosoma cruzi. CD is treated only with benznidazole (Bz) and nifurtimox, both introduced in clinics decades ago despite important limitations, including low efficacy on the later disease stage (chronic form) and severe side effects...
September 1, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28864277/neolignans-from-leaves-of-nectandra-leucantha-lauraceae-display-in%C3%A2-vitro-antitrypanosomal-activity-via-plasma-membrane-and-mitochondrial-damages
#10
Simone S Grecco, Thais A Costa-Silva, Gerold Jerz, Fernanda S de Sousa, Vinicius S Londero, Mariana K Galuppo, Marta L Lima, Bruno J Neves, Carolina H Andrade, Andre G Tempone, João Henrique G Lago
Chagas disease is a neglected tropical disease, caused by the protozoan parasite Trypanosoma cruzi, which affects more than eight million people in Tropical and Subtropical countries especially in Latin America. Current treatment is limited to nifurtimox and benznidazole, both with reduced effectiveness and high toxicity. In this work, the n-hexane extract from leaves of Nectandra leucantha (Lauraceae) displayed in vitro antitrypanosomal activity against T. cruzi. Using several chromatographic steps, four related neolignans were isolated and chemically characterized as dehydrodieugenol B (1), 1-(8-propenyl)-3-[3'-methoxy-1'-(8-propenyl)-phenoxy]-4,5-dimethoxybenzene (2), 1-[(7S)-hydroxy-8-propenyl]-3-[3'-methoxy-1'-(8'-propenyl)-phenoxy]-4-hydroxy-5-methoxybenzene (3), and 1-[(7S)-hydroxy-8-propenyl]-3-[3'-methoxy-1'-(8'-propenyl)-phenoxy]-4,5-dimethoxybenzene (4)...
August 31, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28844141/discovery-and-optimization-of-5-amino-1-2-3-triazole-4-carboxamide-series-against-trypanosoma-cruzi
#11
Stephen Brand, Eun Jung Ko, Elisabet Viayna, Stephen Thompson, Daniel Spinks, Michael Thomas, Lars Sandberg, Amanda F Francisco, Shiromani Jayawardhana, Victoria C Smith, Chimed Jansen, Manu De Rycker, John Thomas, Lorna MacLean, Maria Osuna-Cabello, Jennifer Riley, Paul Scullion, Laste Stojanovski, Frederick R C Simeons, Ola Epemolu, Yoko Shishikura, Sabrinia D Crouch, Tania S Bakshi, Christopher J Nixon, Iain H Reid, Alan P Hill, Tim Z Underwood, Sean J Hindley, Sharon A Robinson, John M Kelly, Jose M Fiandor, Paul G Wyatt, Maria Marco, Timothy J Miles, Kevin D Read, Ian H Gilbert
Chagas' disease, caused by the protozoan parasite Trypanosoma cruzi, is the most common cause of cardiac-related deaths in endemic regions of Latin America. There is an urgent need for new safer treatments because current standard therapeutic options, benznidazole and nifurtimox, have significant side effects and are only effective in the acute phase of the infection with limited efficacy in the chronic phase. Phenotypic high content screening against the intracellular parasite in infected VERO cells was used to identify a novel hit series of 5-amino-1,2,3-triazole-4-carboxamides (ATC)...
September 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28831944/biological-factors-that-impinge-on-chagas-disease-drug-development
#12
Amanda F Francisco, Shiromani Jayawardhana, Michael D Lewis, Martin C Taylor, John M Kelly
Chagas disease is caused by infection with the insect-transmitted protozoan Trypanosoma cruzi, and is the most important parasitic infection in Latin America. The current drugs, benznidazole and nifurtimox, are characterized by limited efficacy and toxic side-effects, and treatment failures are frequently observed. The urgent need for new therapeutic approaches is being met by a combined effort from the academic and commercial sectors, together with major input from not-for-profit drug development consortia...
August 23, 2017: Parasitology
https://www.readbyqxmd.com/read/28795372/development-of-a-pharmacophore-for-cruzain-using-oxadiazoles-as-virtual-molecular-probes-quantitative-structure-activity-relationship-studies
#13
Anacleto S de Souza, Marcelo T de Oliveira, Adriano D Andricopulo
Chagas's is a neglected tropical disease caused by the protozoan parasite Trypanosoma cruzi. According to the World Health Organization, 7 million people are infected worldwide leading to 7000 deaths per year. Drugs available, nifurtimox and benzimidazole, are limited due to low efficacy and high toxicity. As a validated target, cruzain represents a major front in drug discovery attempts for Chagas disease. Herein, we describe the development of 2D QSAR ([Formula: see text] = 0.81) and a 3D-QSAR-based pharmacophore ([Formula: see text] = 0...
August 9, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28690148/betulinic-acid-induces-cell-death-by-necrosis-in-trypanosoma-cruzi
#14
Paloma Leão Sousa, Racquel Oliveira da Silva Souza, Louise Donadello Tessarolo, Ramon Róseo Paula Pessoa Bezerra de Menezes, Tiago Lima Sampaio, Jader Almeida Canuto, Alice Maria Costa Martins
Chagas' disease is a neglected disease caused by the protozoan parasite Trypanosoma cruzi and constitutes a serious health problem worldwide. The treatment is limited, with variable efficacy of benznidazole and nifurtimox. Betulinic Acid (BA), a triterpene, can be found in medicinal herbs and has a wide variety of biological and pharmacological activities. The objective was to evaluate betulinic acid effects on the cell death mechanism in Trypanosoma cruzi strain Y. BA inhibited the growth of epimastigotes in periods of 24h (IC50=73...
October 2017: Acta Tropica
https://www.readbyqxmd.com/read/28652235/nifurtimox-is-ineffective-against-drug-resistant-mycobacteria
#15
LETTER
Mike Marvin Ruth, Jasper Jan Nicolaas Sangen, Heiman Frank Louis Wertheim, Jakko van Ingen
No abstract text is available yet for this article.
September 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28648464/synthesis-and-biological-evaluation-of-2-methyl-1h-benzimidazole-5-carbohydrazides-derivatives-as-modifiers-of-redox-homeostasis-of-trypanosoma-cruzi
#16
Silvia Melchor-Doncel de la Torre, Citlali Vázquez, Zabdi González-Chávez, Lilián Yépez-Mulia, Rocío Nieto-Meneses, Ricardo Jasso-Chávez, Emma Saavedra, Francisco Hernández-Luis
Twelve novel benzimidazole derivatives were synthesized and their in vitro activities against epimastigotes of Trypanosoma cruzi were evaluated. Two derivatives (6 and 7), which have 4-hydroxy-3-methoxyphenyl moiety in their structures, proved to be the most active in inhibiting the parasite growth. Compound 6 showed a trypanocidal activity higher than benznidazole (IC50=5µM and 7.5µM, respectively) and less than nifurtimox (IC50=3.6µM). In addition, the ability of 6 and 7 to modify the redox homeostasis in T cruzi epimastigote was studied; cysteine and glutathione increased in parasites exposed to both compounds, whereas trypanothione only increased with 7 treatment...
August 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28629155/repositioning-fda-drugs-as-potential-cruzain-inhibitors-from-trypanosoma-cruzi-virtual-screening-in-vitro-and-in-vivo-studies
#17
Isidro Palos, Edgar E Lara-Ramirez, Julio Cesar Lopez-Cedillo, Carlos Garcia-Perez, Muhammad Kashif, Virgilio Bocanegra-Garcia, Benjamin Nogueda-Torres, Gildardo Rivera
Chagas disease (CD) is a neglected disease caused by the parasite Trypanosoma cruzi, which affects underdeveloped countries. The current drugs of choice are nifurtimox and benznidazole, but both have severe adverse effects and less effectivity in chronic infections; therefore, the need to discover new drugs is essential. A computer-guided drug repositioning method was applied to identify potential FDA drugs (approved and withdrawn) as cruzain (Cz) inhibitors and trypanocidal effects were confirmed by in vitro and in vivo studies...
June 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28614468/-estimating-demand-for-anti-chagas-drugs-a-contribution-for-access-in-latin-america
#18
Gabriela Costa Chaves, Mariana Abi-Saab Arrieche, Joelle Rode, Daniel Mechali, Priscileyne Ouverney Reis, Renato Vieira Alves, Eric Stobbaerts, Nora Girón Aguilar, Isabela Ribeiro
Objective: Describe a tool to estimate demand for benznidazole and nifurtimox to treat Chagas disease, and report on its implementation in a group of Latin American countries. Methods: The project was carried out in the following stages: 1) development of a tool to estimate demand, and definition of the evaluation and decision variables to estimate demand 2) data collection via a questionnaire completed by representatives of control programs, complemented with data from the literature; 3) presentation of the tool, followed by validation, and adaptation by representatives of the control programs in order to plan drug procurement for 2012 and 2013; and 4) further analysis of the obtained data, especially regarding benznidazole, and comparison of country estimates...
June 8, 2017: Revista Panamericana de Salud Pública, Pan American Journal of Public Health
https://www.readbyqxmd.com/read/28591312/identification-of-a-type-i-nitroreductase-gene-in-non-virulent-trypanosoma-rangeli
#19
Marjorie Montenegro, Claudia Cuervo, Constanza Cardenas, Silvia Duarte, Jenny R Díaz, M Carmen Thomas, Manuel C Lopez, Concepcion J Puerta
Trypanosomatid type I nitroreductases (NTRs), i.e., mitochondrial enzymes that metabolise nitroaromatic pro-drugs, are essential for parasite growth, infection, and survival. Here, a type I NTR of non-virulent protozoan Trypanosoma rangeli is described and compared to those of other trypanosomatids. The NTR gene was isolated from KP1(+) and KP1(-) strains, and its corresponding transcript and 5' untranslated region (5'UTR) were determined. Bioinformatics analyses and nitro-drug activation assays were also performed...
July 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28587855/pheophorbide-a-a-compound-isolated-from-the-leaves-of-arrabidaea-chica-induces-photodynamic-inactivation-of-trypanosoma-cruzi
#20
Nathielle Miranda, Adriana Passarella Gerola, Cláudio Roberto Novello, Tânia Ueda-Nakamura, Sueli de Oliveira Silva, Benedito Prado Dias-Filho, Noboru Hioka, João Carlos Palazzo de Mello, Celso Vataru Nakamura
BACKGROUND: Approximately 6-7 million people are infected with Trypanosoma cruzi, the etiological agent of Chagas' disease. Only two therapeutic compounds have been found to be useful against this disease: nifurtimox and benznidazole. These drugs have been effective in the acute phase of the disease but less effective in the chronic phase; they also have many side effects. Thus, the search for new compounds with trypanocidal action is necessary. Natural products can be the source of many important substances for the development of drugs to treat this infection...
September 2017: Photodiagnosis and Photodynamic Therapy
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