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https://www.readbyqxmd.com/read/29448038/molecular-and-biological-characterization-of-a-highly-pathogenic-trypanosoma-cruzi-strain-isolated-from-a-patient-with-congenital-infection
#1
Julián Ernesto Nicolás Gulin, Margarita Bisio, Daniela Marisa Rocco, Jaime Altcheh, María Elisa Solana, Facundo García-Bournissen
Although many Trypanosoma cruzi (T. cruzi) strains isolated from a wide range of hosts have been characterized, there is a lack of information about biological features from vertically transmitted strains. We describe the molecular and biological characteristics of the T. cruzi VD strain isolated from a congenital Chagas disease patient. The VD strain was typified as DTU TcVI; in vitro sensitivity to nifurtimox (NFX) and beznidazole (BZ) were 2.88 μM and 6.19 μM respectively, while inhibitory concentrations for intracellular amastigotes were 0...
February 12, 2018: Experimental Parasitology
https://www.readbyqxmd.com/read/29340450/therapeutic-drug-monitoring-of-benznidazole-and-nifurtimox-a-systematic-review-and-quality-assessment-of-published-clinical-practice-guidelines
#2
Mario Javier Olivera, Johana Alexandra Fory, Antonio José Olivera
The pharmacological management of adults with chronic-phase Chagas disease is challenging despite it being the recent focus of extensive research. One of the challenges in the current clinical practice guidelines (CPGs) landscape is the existence of non-evidence-based recommendations for the use of laboratory tests in treatment monitoring. This study aimed to systematically assess the quality and consistency of recommendations of CPGs on the pharmacological management of adults with chronic-phase Chagas disease...
November 2017: Revista da Sociedade Brasileira de Medicina Tropical
https://www.readbyqxmd.com/read/29311242/vaccine-linked-chemotherapy-improves-benznidazole-efficacy-for-acute-chagas-disease
#3
Kathryn Jones, Leroy Versteeg, Ashish Damania, Brian Keegan, April Kendricks, Jeroen Pollet, Julio Vladimir Cruz-Chan, Fabian Gusovsky, Peter J Hotez, Maria Elena Bottazzi
Chagas disease affects 6-7 million people worldwide, resulting in significant disease burdens and healthcare costs in endemic countries. Chemotherapeutic treatment is restricted to two parasiticidal drugs benznidazole and nifurtimox. Both drugs are highly effective during acute disease, but are only minimally effective during chronic disease and fraught with significant adverse clinical effects. In experimental models, vaccines can be used to induce parasite specific balanced TH1/TH2 immune responses that effectively reduce parasite burdens and associated inflammation while minimizing adverse effects...
January 8, 2018: Infection and Immunity
https://www.readbyqxmd.com/read/29281643/4-aminopyridyl-based-lead-compounds-targeting-cyp51-prevent-spontaneous-parasite-relapse-in-a-chronic-model-and-improve-cardiac-pathology-in-an-acute-model-of-trypanosoma-cruzi-infection
#4
Claudia Magalhaes Calvet, Jun Yong Choi, Diane Thomas, Brian Suzuki, Ken Hirata, Sharon Lostracco-Johnson, Liliane Batista de Mesquita, Alanderson Nogueira, Marcelo Meuser-Batista, Tatiana Araujo Silva, Jair Lage Siqueira-Neto, William R Roush, Mirian Claudia de Souza Pereira, James H McKerrow, Larissa M Podust
BACKGROUND: Chagas disease, caused by the protozoan Trypanosoma cruzi, is the leading cause of heart failure in Latin America. The clinical treatment of Chagas disease is limited to two 60 year-old drugs, nifurtimox and benznidazole, that have variable efficacy against different strains of the parasite and may lead to severe side effects. CYP51 is an enzyme in the sterol biosynthesis pathway that has been exploited for the development of therapeutics for fungal and parasitic infections...
December 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29247858/investigating-the-structure-activity-relationships-of-n-5-nitrofuran-2-yl-methylene-substituted-hydrazides-against-trypanosoma-cruzi-to-design-novel-active-compounds
#5
Fanny Palace-Berl, Kerly Fernanda Mesquita Pasqualoto, Bianca Zingales, Carolina Borsoi Moraes, Mariana Bury, Caio Haddad Franco, Adelson Lopes da Silva Neto, João Sussumu Murayama, Solange Lessa Nunes, Marcelo Nunes Silva, Leoberto Costa Tavares
Chagas disease, caused by the protozoan Trypanosoma cruzi, is a neglected chronic tropical infection endemic in Latin America. New and effective treatments are urgently needed because the two available drugs - benznidazole (BZD) and nifurtimox (NFX) - have limited curative power in the chronic phase of the disease. We have previously reported the design and synthesis of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides that showed high trypanocidal activity against axenic epimastigote forms of three T...
December 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29113731/oral-fexinidazole-for-late-stage-african-trypanosoma-brucei-gambiense-trypanosomiasis-a-pivotal-multicentre-randomised-non-inferiority-trial
#6
Victor Kande Betu Ku Mesu, Wilfried Mutombo Kalonji, Clélia Bardonneau, Olaf Valverde Mordt, Séverine Blesson, François Simon, Sophie Delhomme, Sonja Bernhard, Willy Kuziena, Jean-Pierre Fina Lubaki, Steven Lumeya Vuvu, Pathou Nganzobo Ngima, Hélène Mahenzi Mbembo, Médard Ilunga, Augustin Kasongo Bonama, Josué Amici Heradi, Jean Louis Lumaliza Solomo, Guylain Mandula, Lewis Kaninda Badibabi, Francis Regongbenga Dama, Papy Kavunga Lukula, Digas Ngolo Tete, Crispin Lumbala, Bruno Scherrer, Nathalie Strub-Wourgaft, Antoine Tarral
BACKGROUND: Few therapeutic options are available to treat the late-stage of human African trypanosomiasis, a neglected tropical disease, caused by Trypanosoma brucei gambiense (g-HAT). The firstline treatment is a combination therapy of oral nifurtimox and intravenous eflornithine that needs to be administered in a hospital setting by trained personnel, which is not optimal given that patients often live in remote areas with few health resources. Therefore, we aimed to assess the safety and efficacy of an oral regimen of fexinidazole (a 2-substituted 5-nitroimidazole with proven trypanocidal activity) versus nifurtimox eflornithine combination therapy in patients with late-stage g-HAT...
January 13, 2018: Lancet
https://www.readbyqxmd.com/read/29084172/benzoic-acid-derivatives-with-trypanocidal-activity-enzymatic-analysis-and-molecular-docking-studies-toward-trans-sialidase
#7
Muhammad Kashif, Antonio Moreno-Herrera, Juan Carlos Villalobos-Rocha, Benjamín Nogueda-Torres, Jaime Pérez-Villanueva, Karen Rodríguez-Villar, José Lius Medina-Franco, Peterson de Andrade, Ivone Carvalho, Gildardo Rivera
Chagas, or American trypanosomiasis, remains an important public health problem in developing countries. In the last decade, trans-sialidase has become a pharmacological target for new anti-Chagas drugs. In this work, the aims were to design and find a new series of benzoic acid derivatives as trans-sialidase (TS) inhibitors and anti-trypanosomal agents. Three compounds (14, 18, and 19) sharing a para-aminobenzoic acid moiety showed more potent trypanocidal activity than the commercially available drugs nifurtimox and benznidazole in both strains: the lysis concentration of 50% of the population (LC50) was <0...
October 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29031078/structural-design-synthesis-and-pharmacological-evaluation-of-thiazoles-against-trypanosoma-cruzi
#8
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...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29016289/experimental-and-clinical-treatment-of-chagas-disease-a-review
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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 7, 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
#17
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)...
November 1, 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
#18
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
#19
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
#20
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...
September 2017: Journal of Computer-aided Molecular Design
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