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https://www.readbyqxmd.com/read/29669503/evaluation-of-trypanocidal-and-antioxidant-activities-of-a-selected-series-of-3-amidocoumarins
#1
Mauricio Moncada-Basualto, Michel Lapier, Juan Diego Maya, Betty Matsuhiro, Claudio Olea-Azar, Giovanna L Delogu, Eugenio Uriarte, Lourdes Santana, Maria Joao Matose
BACKGROUND: Neglected diseases are becoming more prevalent due to globalization. This has inspired active research in the development of new drugs for the treatment of parasitic diseases such as Chagas disease. OBJECTIVES: With the aim of finding new trypanocidal agents, we report the in vitro evaluation of a new series of 3-amidocoumarins with or without hydroxyl substituents at position 4 of the coumarin ring. METHODS: Electrochemical and biological assays were performed in order to assess the antioxidant and trypanocidal potential of these compounds, and to better understand the mechanisms involved in their activity...
April 18, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29588298/severe-immune-thrombocytopaenia-in-a-patient-taking-benznidazole-for-chronic-chagas-disease
#2
Clara Crespillo-Andújar, María Calbacho Robles, Francesca F Norman, Jose A Pérez-Molina
Chagas disease is a parasitic disease that mostly affects Latin American countries, but it has currently become a worldwide epidemic due to migration. Both drugs marketed for its treatment (benznidazole and nifurtimox) are associated with a high rate of adverse reactions. Benznidazole is preferred initially because of its more favourable toxicity profile and perceived greater efficacy. Hypersensitivity dermatological reactions, gastrointestinal and neurological disturbances represent the most common drug-related adverse events...
March 27, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29569658/an-update-on-benznidazole-for-the-treatment-of-patients-with-chagas-disease
#3
R Thakare, A Dasgupta, S Chopra
Chagas disease is a vector-borne, systemic and chronic parasitic infection caused by Trypanosoma cruzi with approximately 8 million cases worldwide. The treatment for acute phase of Chagas disease consists of benznidazole and nifurtimox, although this treatment combination falls short in terms of efficacy against chronic phases of infection. This review provides an update on benznidazole progress and approval by the U.S. Food and Drug Administration in 2017 for the treatment of Chagas disease along with its lacunae...
January 2018: Drugs of Today
https://www.readbyqxmd.com/read/29563916/old-yellow-enzyme-from-trypanosoma-cruzi-exhibits-in-vivo-prostaglandin-f-2-%C3%AE-synthase-activity-and-has-a-key-role-in-parasite-infection-and-drug-susceptibility
#4
Florencia Díaz-Viraqué, María Laura Chiribao, Andrea Trochine, Fabiola González-Herrera, Christian Castillo, Ana Liempi, Ulrike Kemmerling, Juan Diego Maya, Carlos Robello
The discovery that trypanosomatids, unicellular organisms of the order Kinetoplastida, are capable of synthesizing prostaglandins raised questions about the role of these molecules during parasitic infections. Multiple studies indicate that prostaglandins could be related to the infection processes and pathogenesis in trypanosomatids. This work aimed to unveil the role of the prostaglandin F2 α synthase Tc OYE in the establishment of Trypanosoma cruzi infection, the causative agent of Chagas disease. This chronic disease affects several million people in Latin America causing high morbidity and mortality...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29494842/identification-of-cisapride-as-new-inhibitor-of-putrescine-uptake-in-trypanosoma-cruzi-by-combined-ligand-and-structure-based-virtual-screening
#5
R C Dietrich, L N Alberca, M D Ruiz, P H Palestro, C Carrillo, A Talevi, L Gavernet
Nowadays, the pharmacological therapy for the treatment of Chagas disease is based on two old drugs, benznidazole and nifurtimox, which have restricted efficacy against the chronic phase of the illness. To overcome the lack of efficacy of the traditional drugs (and their considerable toxicity), new molecular targets have been studied as starting points to the discovery of new antichagasic compounds. Among them, polyamine transporter TcPAT12 (also known as TcPOT1.1) represents an interesting macromolecule, since polyamines are essential for Trypanosoma cruzi, the parasite that causes the illness, but it cannot synthesize them de novo...
February 13, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29473131/searching-for-new-drugs-for-chagas-diseases-triazole-analogs-display-high-in-vitro-activity-against-trypanosoma-cruzi-and-low-toxicity-toward-mammalian-cells
#6
Robson Xavier Faria, Daniel Tadeu Gomes Gonzaga, Paulo Anastácio Furtado Pacheco, André Luis Almeida Souza, Vitor Francisco Ferreira, Fernando de Carvalho da Silva
Chagas disease is one of the most relevant endemic diseases in Latin America caused by the flagellate protozoan Trypanosoma cruzi. Nifurtimox and benzonidazole are the drugs used in the treatment of this disease, but they commonly are toxic and present severe side effects. New effective molecules, without collateral effects, has promoted the investigation to develop new lead compounds with to advance for clinical trials. Previously, 3-nitro-1H-1,2,4-triazole-based amines and 1,2,3-triazoles demonstrated significant trypanocidal activity against T...
February 23, 2018: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/29471865/a-multicentre-randomised-non-inferiority-clinical-trial-comparing-a-nifurtimox-eflornithine-combination-to-standard-eflornithine-monotherapy-for-late-stage-trypanosoma-brucei-gambiense-human-african-trypanosomiasis-in-uganda
#7
Freddie Kansiime, Seraphine Adibaku, Charles Wamboga, Franklin Idi, Charles Drago Kato, Lawrence Yamuah, Michel Vaillant, Deborah Kioy, Piero Olliaro, Enock Matovu
BACKGROUND: While the combination of nifurtimox and eflornithine (NECT) is currently recommended for the treatment of the late stage human African trypansomiasis (HAT), single-agent eflornithine was still the treatment of choice when this trial commenced. This study intended to provide supportive evidence to complement previous trials. METHODS: A multi-centre randomised, open-label, non-inferiority trial was carried out in the Trypanosoma brucei gambiense endemic districts of North-Western Uganda to compare the efficacy and safety of NECT (200 mg/kg eflornithine infusions every 12 h for 7 days and 8 hourly oral nifurtimox at 5 mg/kg for 10 days) to the standard eflornithine regimen (6 hourly at 100 mg/kg for 14 days)...
February 22, 2018: Parasites & Vectors
https://www.readbyqxmd.com/read/29448038/molecular-and-biological-characterization-of-a-highly-pathogenic-trypanosoma-cruzi-strain-isolated-from-a-patient-with-congenital-infection
#8
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 13, 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
#9
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
#10
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 to 7 million people worldwide, resulting in significant disease burdens and health care costs in countries of endemicity. 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 TH 1/TH 2 immune responses that effectively reduce parasite burdens and associated inflammation while minimizing adverse effects...
April 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
#11
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
#12
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...
January 20, 2018: 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
#13
RANDOMIZED CONTROLLED TRIAL
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
#14
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
#15
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
#16
REVIEW
Policarpo Ademar Sales Junior, Israel Molina, Silvane Maria Fonseca Murta, Adrián Sánchez-Montalvá, Fernando Salvador, Rodrigo Corrêa-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 (BZ) and nifurtimox (NFX). Treatment with these trypanocidal drugs is recommended in both the acute and chronic phases of CD...
November 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
#17
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
#18
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
#19
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
#20
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
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