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https://www.readbyqxmd.com/read/28029081/drug-discovery-for-paediatric-chagas-diseases
#1
Sreekanth Thota, Carlos M Morel
Congenital T. cruzi infection occurs in 1-10% of infants of infected mothers. Treatment of Chagas disease focuses on killing the parasite in acute infection and managing signs and symptoms in later stages. Mothers who test positive should not be treated until they have given birth and have finished breast-feeding. Screening of newborns and other children of infected mothers to provide early diagnosis and treatment. There are only two drugs currently available for the treatment of paediatric chagas disease, nifurtimox and benznidazole...
December 26, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28025938/trypanothione-reductase-and-superoxide-dismutase-as-current-drug-targets-for-trypanosoma-cruzi-an-overview-of-compounds-with-activity-against-chagas-disease
#2
Iván Beltrán-Hortelano, Silvia Pérez-Silanes, Silvia Galiano
It has been over a century since Carlos Chagas discovered the Trypanosoma cruzi (T. cruzi) as the causative agent of Chagas disease (CD), a neglected tropical disease with several socioeconomic, epidemiological and human health repercussions. Currently, there are only two commercialized drugs to treat CD in acute phase, nifurtimox and benznidazol, with several adverse side effects. Thus, new orally available and safe drugs for this parasitic infection are urgently required. One strategy of great importance in new drug discovery programmes is based on the search of molecules enabling to interfere with enzymes involved in T...
December 26, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28011170/antiprotozoal-drug-nitazoxanide-enhances-parasitemia-tissue-lesions-and-mortality-caused-by-trypanosoma-cruzi-in-murine-model
#3
Juan Salvador Valle-Reyes, Valery Melnikov, Oxana Dobrovinskaya, Alejandrina Rodriguez-Hernández, Cristina Wookee-Zea, Víctor Pimientel-Rodrigez, Gabriela Rueda-Valdovinos, Iván Delgado-Enciso, Uriel A López-Lemus, Francisco Espinoza-Gómez
Chagas' disease is caused by unicellular parasite Trypanosoma cruzi (T. cruzi). It is endemic throughout Latin America, but nowadays has become a global challenge due to tourism and migration. Non-treated infection may result in health-threatening complications and lead to death. Current medications for this infection are nifurtimox (NFT) and benznidazol. Both drugs may cause side effects and are ineffective in the chronic phase. Therefore, new antichagasic compounds are urgently required. Nitazoxanide (NTZ) is a broad spectrum antiparasitic drug, proposed recently as a potential candidate to be added to the list of essential medicines for integrated neglected tropical disease control and elimination...
December 21, 2016: Experimental Parasitology
https://www.readbyqxmd.com/read/27951486/in%C3%A2-vitro-activity-and-mode-of-action-of-distamycin-analogues-against-african-trypanosomes
#4
Jaime Franco, Andrea Medeiros, Diego Benítez, Karen Perelmuter, Gloria Serra, Marcelo A Comini, Laura Scarone
Distamycin, a natural polyamide containing three heterocycle rings with a polar end, has inspired several groups to prepare synthetic analogues, which proved to have anti-trypanosomal and anti-tumoral activity. We describe the synthesis of bi and tri thiazoles amides that harbor different substitutions at their ends and the evaluation of their anti-Trypanosoma brucei activity. The most active compound 10b showed better biological activity (EC50 310 nM and selectivity index 16) than the control drug nifurtimox (EC50 15 μM and selectivity index 10)...
December 2, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27908757/synthesis-antioxidant-and-antichagasic-properties-of-a-selected-series-of-hydroxy-3-arylcoumarins
#5
Natalia Robledo-O'Ryan, Maria João Matos, Saleta Vazquez-Rodriguez, Lourdes Santana, Eugenio Uriarte, Mauricio Moncada-Basualto, Francisco Mura, Michel Lapier, Juan Diego Maya, Claudio Olea-Azar
Oxidative stress is involved in several parasitic diseases such as Chagas. Agents able to selectively modulate biochemical processes involved in the disease represent promising multifunctional agents for the delay or abolishment of the progression of this pathology. In the current work, differently substituted hydroxy-3-arylcoumarins are described, exerting both antioxidant and trypanocidal activity. Among the compounds synthesized, compound 8 showed the most interesting profile, presenting a moderate scavenging ability for peroxyl radicals (ORAC-FL=2...
January 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27908747/tci-tcii-and-tcvi-trypanosoma-cruzi-samples-from-chagas-disease-patients-with-distinct-clinical-forms-and-critical-analysis-of-in-vitro-and-in-vivo-behavior-response-to-treatment-and-infection-evolution-in-murine-model
#6
Maykon Tavares de Oliveira, Renata Tupinambá Branquinho, Gláucia Diniz Alessio, Carlos Geraldo Campos Mello, Nívia Carolina Nogueira-de-Paiva, Cláudia Martins Carneiro, Max Jean de Ornelas Toledo, Alexandre Barbosa Reis, Olindo Assis Martins Martins-Filho, Marta de Lana
The clonal evolution of Trypanosoma cruzi sustains scientifically the hypothesis of association between parasite's genetic, biological behavior and possibly the clinical aspects of Chagas disease in patients from whom they were isolated. This study intended to characterize a range of biological properties of TcI, TcII and TcVI T. cruzi samples in order to verify the existence of these associations. Several biological features were evaluated, including in vitro epimastigote-growth, "Vero"cells infectivity and growth, along with in vivo studies of parasitemia, polymorphism of trypomastigotes, cardiac inflammation, fibrosis and response to treatment by nifurtimox during the acute and chronic murine infection...
November 28, 2016: Acta Tropica
https://www.readbyqxmd.com/read/27855164/trypanosoma-brucei-cyp51-essentiality-and-targeting-therapy-in-an-experimental-model
#7
Frédéric-Antoine Dauchy, Mélanie Bonhivers, Nicolas Landrein, Denis Dacheux, Pierrette Courtois, Florian Lauruol, Sylvie Daulouède, Philippe Vincendeau, Derrick R Robinson
Trypanosoma brucei gambiense is the main causative agent of Human African Trypanosomiasis (HAT), also known as sleeping sickness. Because of limited alternatives and treatment toxicities, new therapeutic options are urgently needed for patients with HAT. Sterol 14alpha-demethylase (CYP51) is a potential drug target but its essentiality has not been determined in T. brucei. We used a tetracycline-inducible RNAi system to assess the essentiality of CYP51 in T. brucei bloodstream form (BSF) cells and we evaluated the effect of posaconazole, a well-tolerated triazole drug, within a panel of virulent strains in vitro and in a murine model...
November 2016: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/27812217/activation-of-bicyclic-nitro-drugs-by-a-novel-nitroreductase-ntr2-in-leishmania
#8
Susan Wyllie, Adam J Roberts, Suzanne Norval, Stephen Patterson, Bernardo J Foth, Matthew Berriman, Kevin D Read, Alan H Fairlamb
Drug discovery pipelines for the "neglected diseases" are now heavily populated with nitroheterocyclic compounds. Recently, the bicyclic nitro-compounds (R)-PA-824, DNDI-VL-2098 and delamanid have been identified as potential candidates for the treatment of visceral leishmaniasis. Using a combination of quantitative proteomics and whole genome sequencing of susceptible and drug-resistant parasites we identified a putative NAD(P)H oxidase as the activating nitroreductase (NTR2). Whole genome sequencing revealed that deletion of a single cytosine in the gene for NTR2 that is likely to result in the expression of a non-functional truncated protein...
November 2016: PLoS Pathogens
https://www.readbyqxmd.com/read/27784255/clear-shot-at-primary-aim-susceptibility-of-trypanosoma-cruzi-organelles-structures-and-molecular-targets-to-drug-treatment
#9
Rubem Figueiredo Sadok Menna-Barreto, Solange Lisboa de Castro
Chagas disease, caused by Trypanosoma cruzi, stands out due to its socio- economic effects on low-income tropical populations. This disease affects millions of people worldwide. The current chemotherapy for it is based on benznidazole (Bz) and nifurtimox (Nif) and is unsatisfactory. In this review, we will focus on the search for potential target organelles and molecules for the chemotherapy of Chagas disease. We consider as potential target organelles those that are absent or significantly different in host cells and present in the clinically relevant forms of the parasite (trypomastigotes and amastigotes), which are the mitochondrion, cytoskeletal- related structures, the acidocalcisomes/contractile vacuole complex and glycosomes...
October 25, 2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/27784230/targets-and-patented-drugs-for-chemotherapy-of-chagas-disease-in-the-last-15-years-period
#10
Vilma G Duschak
The American trypanosomiasis, Chagas disease, is a parasitic infection typically spread by triatomine vectors affecting millions of people all over Latin America. Existing chemotherapy is centered on the nitroaromatic compounds benznidazole and nifurtimox that provide unsatisfactory results and substantial side effects. So, the finding and exploration of novel ways to challenge this neglected disease is a main priority. The biologic and biochemical progress in the scientific knowledge of Trypanosoma cruzi in the period comprising the last 15-years, has increased the identification of multiple targets for Chagas´ disease chemotherapy...
October 24, 2016: Recent Patents on Anti-infective Drug Discovery
https://www.readbyqxmd.com/read/27748443/nitroheterocyclic-drugs-cure-experimental-trypanosoma-cruzi-infections-more-effectively-in-the-chronic-stage-than-in-the-acute-stage
#11
Amanda Fortes Francisco, Shiromani Jayawardhana, Michael D Lewis, Karen L White, David M Shackleford, Gong Chen, Jessica Saunders, Maria Osuna-Cabello, Kevin D Read, Susan A Charman, Eric Chatelain, John M Kelly
The insect-transmitted protozoan parasite Trypanosoma cruzi is the causative agent of Chagas disease, and infects 5-8 million people in Latin America. Chagas disease is characterised by an acute phase, which is partially resolved by the immune system, but then develops as a chronic life-long infection. There is a consensus that the front-line drugs benznidazole and nifurtimox are more effective against the acute stage in both clinical and experimental settings. However, confirmative studies have been restricted by difficulties in demonstrating sterile parasitological cure...
October 17, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27694095/anterior-uveitis-as-the-first-sign-of-human-african-trypanosomiasis-a-case-report
#12
L N Nsiangani, D Kaimbo Wa Kaimbo, M L Kazumba
We report the case of a 13-year-old girl who consulted for blurred vision, pain, and redness in her left eye. Ophthalmologic examination revealed chronic, hypertensive, and non-granulomatous anterior uveitis. The disease course was marked by a reversal of diurnal rhythm, with daytime sleepiness and behavioral disorders. A neuropsychiatric examination suggested human African trypanosomiasis (HAT), or sleeping sickness. The diagnosis was confirmed by the detection of Trypanosoma in the cerebrospinal fluid. The NECT regimen (nifurtimox-eflornithine combination therapy) was administered as medical treatment and resulted in the disappearance of all clinical signs...
August 1, 2016: Médecine et Santé Tropicales
https://www.readbyqxmd.com/read/27639944/assessing-anti-t-%C3%A2-cruzi-candidates-in%C3%A2-vitro-for-sterile-cidality
#13
Monica Cal, Jean-Robert Ioset, Matthia A Fügi, Pascal Mäser, Marcel Kaiser
Total clearance of the T. cruzi infection - referred to herein as "sterile cure" - seems to be a critical prerequisite for new drug candidates for Chagas disease, ensuring long-term beneficial effects for patients in the chronic indeterminate stage. This requirement is notably supported by the recent findings of clinical studies involving posaconazole and fosravuconazole, where the majority of patients treated eventually relapsed after an apparent clearance of parasitaemia at the end of treatment. We have adapted an in vitro system to predict the ability of a compound to deliver sterile cure...
December 2016: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/27599261/antiparasitic-activity-of-diterpenoids-against-trypanosoma-cruzi
#14
Sergio Alegre-Gómez, Paula Sainz, M Fátima Simões, Patrícia Rijo, Cristina Moiteiro, Azucena González-Coloma, Rafael A Martínez-Díaz
Twenty-seven diterpenes, including abietanes, labdanes, abeoabietanes, halimanes, and pimaranes, have been evaluated against epimastigote and intracellular amastigote forms of Trypanosoma cruzi and also against LC5 and NCTC cell lines. Royleanones (3, 4, and 5) and a further abietane (12), obtained by purification of Plectranthus spp. extracts, were the most active compounds on epimastigotes, showing IC50 values similar (1.73 µg/mL, 12) or even lower (0.39, 0.99, and 1.20 µg/mL, 3, 4, and 5 respectively) than the positive control nifurtimox (2...
September 6, 2016: Planta Medica
https://www.readbyqxmd.com/read/27558676/flavonoids-and-chagas-disease-the-story-so-far
#15
Seyed Fazel Nabavi, Antoni Sureda, Maria Daglia, Morteza Izadi, Eduardo Sobarzo-Sánchez, Luca Rastrelli, Seyed Mohammad Nabavi
Chagas disease is one of the major health problems in Central and South America, which is caused by the parasitic protozoa, Trypanosoma cruzi. It is commonly transmitted by members of blood-sucking subfamily Triatominae. Chagas disease is associated with cardiac and gastrointestinal manifestations. Up to now, there are no effective vaccines for the treatment of Chagas disease and benznidazole and nifurtimox are as the only effective anti-Chagas drugs that cause different adverse and side effects. Therefore, much attention has been paid to natural products as novel therapeutic strategies for Chagas disease and its manifestations...
August 24, 2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/27551855/differential-gel-electrophoresis-dige-evaluation-of-naphthoimidazoles-mode-of-action-a-study-in-trypanosoma-cruzi-bloodstream-trypomastigotes
#16
Giselle Villa Flor Brunoro, Vitor Marcel Faça, Marcelle Almeida Caminha, André Teixeira da Silva Ferreira, Monique Trugilho, Kelly Cristina Gallan de Moura, Jonas Perales, Richard Hemmi Valente, Rubem Figueiredo Sadok Menna-Barreto
BACKGROUND: The obligate intracellular protozoan Trypanosoma cruzi is the causative agent of Chagas disease, a neglected illness affecting millions of people in Latin America that recently entered non-endemic countries through immigration, as a consequence of globalization. The chemotherapy for this disease is based mainly on benznidazole and nifurtimox, which are very efficient nitroderivatives against the acute stage but present limited efficacy during the chronic phase. Our group has been studying the trypanocidal effects of naturally occurring quinones and their derivatives, and naphthoimidazoles derived from β-lapachone N1, N2 and N3 were the most active...
August 2016: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/27491458/zoonotic-trypanosomes-in-south-east-asia-attempts-to-control-trypanosoma-lewisi-using-human-and-animal-trypanocidal-drugs
#17
Marc Desquesnes, Sarawut Yangtara, Pawinee Kunphukhieo, Sathaporn Jittapalapong, Stéphane Herder
Beside typical human trypanosomes responsible of sleeping sickness in Africa and Chagas disease in Latin America, there is a growing number of reported atypical human infections due to Trypanosoma evansi, a livestock parasite, or Trypanosoma lewisi, a rat parasite, especially in Asia. Drugs available for the treatment of T. brucei ssp. in humans are obviously of choice for the control of T. evansi because it is derived from T. brucei. However, concerning T. lewisi, there is an urgent need to determine the efficacy of trypanocidal drugs for the treatment in humans...
October 2016: Infection, Genetics and Evolution
https://www.readbyqxmd.com/read/27460450/the-characterization-of-anti-t-cruzi-activity-relationships-between-ferrocenyl-cyrhetrenyl-complexes-and-ros-release
#18
César Echeverría, Valentina Romero, Rodrigo Arancibia, Hugo Klahn, Ignacio Montorfano, Ricardo Armisen, Vincenzo Borgna, Felipe Simon, Rodrigo Ramirez-Tagle
Trypanosoma cruzi (T. cruzi) is the parasite that causes Chagas disease. Nifurtimox is the most used drug against the T. cruzi, this drug increases intermediaries nitro group, being mainly responsible for the high toxicity component, for this reason it is important to study new organic compounds and thus improve therapeutic strategies against Chagas disease. The electronic effects of ferrocenyl and cyrhetrenyl fragments were investigated by DFT calculation. A close correlation was found between HOMO-LUMO gap of nitro radical NO 2 (-) with the experimental reduction potential found for nitro group and IC50 of two forms the T...
August 2016: Biometals: An International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine
https://www.readbyqxmd.com/read/27432838/safety-profile-of-nifurtimox-for-treatment-of-chagas-disease-in-the-united-states
#19
Colin J Forsyth, Salvador Hernandez, Wilman Olmedo, Adieb Abuhamidah, Mahmoud I Traina, Daniel R Sanchez, Jonathan Soverow, Sheba K Meymandi
BACKGROUND: Nifurtimox is 1 of only 2 medications available for treating Chagas disease (CD) and currently the only drug available in the United States, but its safety and tolerance have not been extensively studied. This is the first study to evaluate tolerance of nifurtimox in US patients with CD. METHODS: This investigation assessed side effects in a sample of 53 patients with CD, all Latin American immigrants, who underwent treatment with nifurtimox (8-10 mg/kg in 3 daily doses for 12 weeks) from March 2008 to July 2012...
October 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27396731/synthesis-biological-evaluation-and-molecular-docking-of-new-benzenesulfonylhydrazone-as-potential-anti-trypanosoma-cruzi-agents
#20
Silvia Elizondo-Jimenez, Antonio Moreno-Herrera, Rogelio Reyes-Olivares, Edith Dorantes-Gonzalez, Benjamín Nogueda-Torres, Eduardo Alves Gamosa de Oliveira, Nelilma C Romeiro, Lidia Moreira Lima, Isidro Palos, Gildardo Rivera
BACKGROUND: Chagas disease is a public health problem caused by Trypanosoma cruzi. Cruzain is a pharmacological target for designing a new drug against this parasite. Hydrazone and N-acylhydrazone derivatives have been traditionally associated as potential Cruzain inhibitors. Additionally, benzenesulfonyl derivatives show trypanocidal activity. Therefore, in this study, the combination of both structures has been taken into account for drug design. METHODS: Seven benzenesulfonylhydrazone (BS-H) and seven N-propionyl benzenesulfonylhydrazone (BS-NAH) derivatives were synthetized and elucidated by infrared spectroscopy, nuclear magnetic resonance, and elemental analysis...
June 30, 2016: Medicinal Chemistry
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