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Relevant bibliographies by topics / Trypanocidal Agents

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Academic literature on the topic 'Trypanocidal Agents'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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Journal articles on the topic "Trypanocidal Agents"

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O'Shea, Ivan P., Mohammed Shahed, Benjamín Aguilera-Venegas, and Shane R. Wilkinson. "Evaluating 5-Nitrothiazoles as Trypanocidal Agents." Antimicrobial Agents and Chemotherapy 60, no. 2 (2015): 1137–40. http://dx.doi.org/10.1128/aac.02006-15.

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ABSTRACTThe growth-inhibitory properties of a 5-nitrothiazole series were evaluated againstTrypanosoma brucei. A subset of related compounds displayed the greatest potency toward the parasite while exhibiting little cytotoxic effect on mammalian cells, with this antiparasitic activity dependent on expression of a type I nitroreductase by the trypanosome. We conclude that the 5-nitrothiazole class of nitroheterocyclic drugs may represent a new lead in the treatment of human African trypanosomiasis.

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Bot, Christopher, Belinda S. Hall, Guzmán Álvarez, et al. "Evaluating 5-Nitrofurans as Trypanocidal Agents." Antimicrobial Agents and Chemotherapy 57, no. 4 (2013): 1638–47. http://dx.doi.org/10.1128/aac.02046-12.

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ABSTRACTThe nitroheterocycle nifurtimox, as part of a nifurtimox-eflornithine combination therapy, represents one of a limited number of treatments targetingTrypanosoma brucei, the causative agent of human African trypanosomiasis. The mode of action of this prodrug involves an initial activation reaction catalyzed by a type I nitroreductase (NTR), an enzyme found predominantly in prokaryotes, leading to the formation of a cytotoxic unsaturated open-chain nitrile metabolite. Here, we evaluate the trypanocidal activities of a library of other 5-nitrofurans against the bloodstream form ofT. bruce

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Capes, Amy, Stephen Patterson, Susan Wyllie, et al. "Quinol derivatives as potential trypanocidal agents." Bioorganic & Medicinal Chemistry 20, no. 4 (2012): 1607–15. http://dx.doi.org/10.1016/j.bmc.2011.12.018.

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Harrington, John M., Chris Scelsi, Andreas Hartel, et al. "Novel African Trypanocidal Agents: Membrane Rigidifying Peptides." PLoS ONE 7, no. 9 (2012): e44384. http://dx.doi.org/10.1371/journal.pone.0044384.

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Suganuma, Keisuke, Albertus Eka Yudistira Sarwono, Shinya Mitsuhashi, et al. "Mycophenolic Acid and Its Derivatives as Potential Chemotherapeutic Agents Targeting Inosine Monophosphate Dehydrogenase in Trypanosoma congolense." Antimicrobial Agents and Chemotherapy 60, no. 7 (2016): 4391–93. http://dx.doi.org/10.1128/aac.02816-15.

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ABSTRACTThis study aimed to evaluate the trypanocidal activity of mycophenolic acid (MPA) and its derivatives forTrypanosoma congolense. The proliferation ofT. congolensewas completely inhibited by adding <1 μM MPA and its derivatives. In addition, the IMP dehydrogenase inT. congolensewas molecularly characterized as the target of these compounds. The results suggest that MPA and its derivatives have the potential to be new candidates as novel trypanocidal drugs.

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Soulère, Laurent, Pascal Hoffmanna, and Frédéric Bringaud. "Synthesis of sydnonimine derivatives as potential trypanocidal agents." Journal of Heterocyclic Chemistry 40, no. 5 (2003): 943–47. http://dx.doi.org/10.1002/jhet.5570400533.

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Kasozi, Keneth Iceland, Ewan Thomas MacLeod, and Susan Christina Welburn. "Systematic Review and Meta-Analysis on Human African Trypanocide Resistance." Pathogens 11, no. 10 (2022): 1100. http://dx.doi.org/10.3390/pathogens11101100.

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Background Human African trypanocide resistance (HATr) is a challenge for the eradication of Human African Trypansomiaisis (HAT) following the widespread emergence of increased monotherapy drug treatment failures against Trypanosoma brucei gambiense and T. b. rhodesiense that are associated with changes in pathogen receptors. Methods: Electronic searches of 12 databases and 3 Google search websites for human African trypanocide resistance were performed using a keyword search criterion applied to both laboratory and clinical studies. Fifty-one publications were identified and included in this

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Ortiz-Pérez, Eyra, Adriana Moreno-Rodríguez, Timoteo Delgado-Maldonado, et al. "Repositioning FDA-Approved Sulfonamide-Based Drugs as Potential Carbonic Anhydrase Inhibitors in Trypanosoma cruzi: Virtual Screening and In Vitro Studies." Pharmaceuticals 18, no. 5 (2025): 669. https://doi.org/10.3390/ph18050669.

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Background/Objectives: α-carbonic anhydrase (α-TcCA) has emerged as a promising drug target in T. cruzi, the causative agent of Chagas disease in the Americas. Sulfonamides, known inhibitors of CAs, bind to the zinc ion on the enzyme’s active site. This study proposes the repositioning of sulfonamide-based drugs to identify new trypanocidal agents. Method: Ligand-based virtual screening and molecular docking analysis were performed on FDA-approved drugs targeting α-TcCA. These compounds were evaluated in vitro and ex vivo against the A1 and NINOA strains, followed by enzymatic assays. Results:

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Bot, Chris, Belinda S. Hall, Noosheen Bashir, Martin C. Taylor, Nuala A. Helsby, and Shane R. Wilkinson. "Trypanocidal Activity of Aziridinyl Nitrobenzamide Prodrugs." Antimicrobial Agents and Chemotherapy 54, no. 10 (2010): 4246–52. http://dx.doi.org/10.1128/aac.00800-10.

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ABSTRACT The trypanocidal agents nifurtimox and benznidazole both function as prodrugs and must undergo enzyme-mediated activation, a reaction catalyzed by type I nitroreductase (NTR). In the search for new parasitic therapies, we have utilized this finding to investigate whether aziridinyl nitrobenzamide derivatives have activity against bloodstream-form Trypanosoma brucei and Trypanosoma cruzi amastigotes, parasite stages that replicate in the mammalian host. For T. cruzi drug screening, we generated trypanosomes that expressed the luciferase reporter gene and optimized a mammalian infection

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Sufrin, Janice R., Arthur J. Spiess, Canio J. Marasco, Donna Rattendi, and Cyrus J. Bacchi. "Novel Trypanocidal Analogs of 5′-(Methylthio)-Adenosine." Antimicrobial Agents and Chemotherapy 52, no. 1 (2007): 211–19. http://dx.doi.org/10.1128/aac.00480-07.

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ABSTRACT The purine nucleoside 5′-deoxy-5′-(hydroxyethylthio)-adenosine (HETA) is an analog of the polyamine pathway metabolite 5′-deoxy-5′-(methylthio)-adenosine (MTA). HETA is a lead structure for the ongoing development of selectively targeted trypanocidal agents. Thirteen novel HETA analogs were synthesized and examined for their in vitro trypanocidal activities against bloodstream forms of Trypanosoma brucei brucei LAB 110 EATRO and at least one drug-resistant Trypanosoma brucei rhodesiense clinical isolate. New compounds were also assessed in a cell-free assay for their activities as sub

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Dissertations / Theses on the topic "Trypanocidal Agents"

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Mugoyela, Veronica Kapesa. "The design and synthesis of novel trypanocidal agents." Thesis, University of Sunderland, 1990. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.314809.

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ALVES, Alinne Élida Gonçalves. "Obtenção de sistema microparticulado benznidazol: ZIF-8 para liberação prolongada otimizando o tratamento da doença de Chagas." Universidade Federal de Pernambuco, 2016. https://repositorio.ufpe.br/handle/123456789/18704.

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Submitted by Irene Nascimento (irene.kessia@ufpe.br) on 2017-05-04T18:15:26Z No. of bitstreams: 2 license_rdf: 1232 bytes, checksum: 66e71c371cc565284e70f40736c94386 (MD5) Dissertação-Final (5).pdf: 1546136 bytes, checksum: 53adafdfff412dd5657ebbb3bab08a78 (MD5)<br>Made available in DSpace on 2017-05-04T18:15:26Z (GMT). No. of bitstreams: 2 license_rdf: 1232 bytes, checksum: 66e71c371cc565284e70f40736c94386 (MD5) Dissertação-Final (5).pdf: 1546136 bytes, checksum: 53adafdfff412dd5657ebbb3bab08a78 (MD5) Previous issue date: 2016-02-24<br>O benznidazol (BNZ) é um derivado de 2-nitroimida

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Barros, Luiz Marivando. "Constituintes químicos e propriedades bioativas de Lantana montevidensis (spreng.) briq. e Lantana camara L. (verbenaceae): evidências para o uso farmacológico." Universidade Federal de Santa Maria, 2016. http://repositorio.ufsm.br/handle/1/4499.

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Humans have been using medicinal plants for centuries as preventive or curative agents. In Brazil, the use of plants in the treatment of diseases is influenced by Indigenous, African and European cultures. Among these plants are Lantana camara and L. montevidensis commonly known as camará-de-cheiro and chumbinho , respectively. They are used in the North-eastern part of Brazil as tonic sudorific and febrifuge agent. They are also used against, coughs, bronchitis, rheumatism, asthma, ulcer and microbial infections. Considering that there is limited therapy against Leishmaniasis and Try

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Traoré, Moussa. "Contribution à la synthèse et à l'étude du mécanisme d'action de nouveaux agents trypanocides et anticancéreux." Toulouse 3, 1990. http://www.theses.fr/1990TOU3O201.

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La these a pour objet la synthese et l'etude de molecules biologiquement actives a la fois en tant qu'antiparasitaires et anticancereux. Cette dualite tient au fait que trypanosomes et cellules cancereuses presentent un certain nombre de similitudes dans leurs cycles biologiques, liees en particulier a la frequence elevee de leur division; ces similitudes sont presentees dans une introduction generale. La premiere partie consacree aux trypanosomiases, donne tout d'abord une presentation de ces parasitoses, en particulier maladie du sommeil, soulignant les limites des therapies actuelles et les

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Betbeder, Didier. "Synthese et etude du mode d'action d'inhibiteurs de voies metaboliques du trypanosome." Toulouse 3, 1988. http://www.theses.fr/1988TOU30029.

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Etude d'inhibiteurs de voies metaboliques du trypanosome. Synthese et action d'inhibiteurs possibles d'enzymes de replication. Etude d'enzymes de la glycolyse, cible cle dans le trypanosome, celui-ci utilisant le glucose comme seule source d'energie. Puis caracterisation d'une proteine qui presente les proprietes de recepteur vis-a-vis d'une nouvelle famille de trypanocides derives du diphenyl methane

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Defaux, J., M. Sala, X. Formosa, et al. "Huprines as a new family of dual acting trypanocidal–antiplasmodial agents." 2011. http://hdl.handle.net/10454/7468.

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No<br>A series of 19 huprines has been evaluated for their activity against cultured bloodstream forms of Trypanosoma brucei and Plasmodium falciparum. Moreover, cytotoxicity against rat myoblast L6 cells was assessed for selected huprines. All the tested huprines are moderately potent and selective trypanocidal agents, exhibiting IC50 values against T. brucei in the submicromolar to low micromolar range and selectivity indices for T. brucei over L6 cells of approximately 15, thus constituting interesting trypanocidal lead compounds. Two of these huprines were also found to be active against a

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Sola, I., S. Castellà, E. Viayna, et al. "Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal–antiplasmodial activity." 2015. http://hdl.handle.net/10454/7485.

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Yes<br>Dual submicromolar trypanocidal–antiplasmodial compounds have been identified by screening and chemical synthesis of 4-aminoquinoline-based heterodimeric compounds of three different structural classes. In Trypanosoma brucei, inhibition of the enzyme trypanothione reductase seems to be involved in the potent trypanocidal activity of these heterodimers, although it is probably not the main biological target. Regarding antiplasmodial activity, the heterodimers seem to share the mode of action of the antimalarial drug chloroquine, which involves inhibition of the haem detoxification proces

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Sola, I., A. Artigas, M. C. Taylor, et al. "Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines." 2014. http://hdl.handle.net/10454/7496.

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We have synthesized a series of dimers of (+)-(7R,11R)-huprine Y and evaluated their activity against Trypanosoma brucei, Plasmodium falciparum, rat myoblast L6 cells and human acetylcholinesterase (hAChE), and their brain permeability. Most dimers have more potent and selective trypanocidal activity than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain active against hAChE. Lead optimization will focus on identifying compounds with a more favourable trypanocidal/anticholinesterase activity ratio.

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