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Journal articles on the topic 'Trypanocidal Agents'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

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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3

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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4

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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5

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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6

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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7

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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8

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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9

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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10

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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11

Dias, Gleiston G., Torben Rogge, Rositha Kuniyil, et al. "Ruthenium-catalyzed C–H oxygenation of quinones by weak O-coordination for potent trypanocidal agents." Chemical Communications 54, no. 91 (2018): 12840–43. http://dx.doi.org/10.1039/c8cc07572g.

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12

Gordhan, Heeren M., Stephen L. Patrick, Maria I. Swasy, et al. "Evaluation of substituted ebselen derivatives as potential trypanocidal agents." Bioorganic & Medicinal Chemistry Letters 27, no. 3 (2017): 537–41. http://dx.doi.org/10.1016/j.bmcl.2016.12.021.

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13

Granero, Gladys E., María M. de Bertorello, and Margarita C. Briñón. "Synthesis of New Isoxazolylnaphthoquinones as Potential Trypanocidal and Antibacterial Agents." Journal of Chemical Research 23, no. 2 (1999): 110–11. http://dx.doi.org/10.1177/174751989902300222.

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14

Cerecetto, H., R. Di Maio, G. Seoane, C. Ochoa, A. Gómez-Barrio, and S. Muelas. "Synthesis of 1,2,6-Thiadiazin 1,1-Dioxide Derivatives as Trypanocidal Agents." Molecules 5, no. 12 (2000): 499–500. http://dx.doi.org/10.3390/50300499.

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15

Muschietti, Liliana V., and Jerónimo L. Ulloa. "Natural Sesquiterpene Lactones as Potential Trypanocidal Therapeutic Agents: A Review." Natural Product Communications 11, no. 10 (2016): 1934578X1601101. http://dx.doi.org/10.1177/1934578x1601101036.

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Chagas’ disease and Human African Trypanosomiasis are parasitic diseases that remain major health problems, mainly among the poorest and the most marginalized communities from Latin America and Africa. The scarcity of effective chemotherapy, due to the low investment in the research and development (R&D) of new drugs, together with a high incidence of side effects, and the emergence of drug resistance phenomena emphasize the urgent need for new prophylactic and therapeutic agents. Over the ages, humans have employed natural products to treat a wide spectrum of diseases. Recently, the pharm

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16

Moshiri, Houtan, Vaibhav Mehta, Chun Wai Yip, and Reza Salavati. "Pilot-Scale Compound Screening against RNA Editing Identifies Trypanocidal Agents." Journal of Biomolecular Screening 20, no. 1 (2014): 92–100. http://dx.doi.org/10.1177/1087057114548833.

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Most mitochondrial messenger RNAs in trypanosomatid pathogens undergo a unique type of posttranscriptional modification involving insertion and/or deletion of uridylates. This process, RNA editing, is catalyzed by a multiprotein complex (~1.6 MDa), the editosome. Knockdown of core editosome proteins compromises mitochondrial function and, ultimately, parasite viability. Hence, because the editosome is restricted to trypanosomatids, it serves as a unique drug target in these pathogens. Currently, there is a lack of editosome inhibitors for antitrypanosomatid drug development or that could serve

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17

Granero, Gladys E., Maríía M. de Bertorello, and Margarita C. Brin˜ón. "Synthesis of New Isoxazolylnaphthoquinones as Potential Trypanocidal and Antibacterial Agents." Journal of Chemical Research, no. 2 (1999): 110–11. http://dx.doi.org/10.1039/a806065g.

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18

Tapia, Ricardo A., Claudia Carrasco, Scarlet Ojeda, et al. "Synthesis of indazol-4,7-dione derivatives as potential trypanocidal agents." Journal of Heterocyclic Chemistry 39, no. 5 (2002): 1093–96. http://dx.doi.org/10.1002/jhet.5570390540.

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19

Lunardi, Fabiane, Michel Guzela, Andrea T. Rodrigues, et al. "Trypanocidal and Leishmanicidal Properties of Substitution-Containing Chalcones." Antimicrobial Agents and Chemotherapy 47, no. 4 (2003): 1449–51. http://dx.doi.org/10.1128/aac.47.4.1449-1451.2003.

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ABSTRACT Ten chalcones were synthesized and tested as potential leishmanicidal and trypanocidal agents. All tested compounds caused concentration-dependent inhibition of the in vitro growth of Leishmania braziliensis and Trypanosoma cruzi with no significant toxic effect towards host macrophages. Our results show that the positions of the substituents seem to be critical for their antiprotozoal activities.

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20

Gómez-Escobedo, Rogelio, Domingo Méndez-Álvarez, Citlali Vázquez, et al. "Molecular Docking-Based Virtual Screening of FDA-Approved Drugs Using Trypanothione Reductase Identified New Trypanocidal Agents." Molecules 29, no. 16 (2024): 3796. http://dx.doi.org/10.3390/molecules29163796.

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American trypanosomiasis or Chagas disease, caused by Trypanosoma cruzi (T. cruzi), affects approximately 6–7 million people worldwide. However, its pharmacological treatment causes several uncomfortable side effects, causing patients’ treatment abandonment. Therefore, there is a need for new and better treatments. In this work, the molecular docking of nine hundred twenty-four FDA-approved drugs on three different sites of trypanothione reductase of T. cruzi (TcTR) was carried out to find potential trypanocidal agents. Finally, biological evaluations in vitro and in vivo were conducted with t

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21

Onyeyili, P. A., and K. Aliyoo. "In vitro and in vivo evaluation of antitrypanosomal activity of Annona muricata stem bark extracts." Herba Polonica 61, no. 2 (2015): 50–62. http://dx.doi.org/10.1515/hepo-2015-0015.

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Summary The control of trypanosomosis in animals and humans based on chemotherapy is limited and not ideal, since the agents used are associated with severe side effects, and emergence of relapse and drug resistant parasites. The need for the development of new, cheap and safe compounds stimulated this study. Three concentrations (211, 21.1 and 2.11 mg per ml) of chloroform stem bark extract of Annona muricata were screened for trypanocidal activity against Trypanosoma brucei brucei in vitro. Also, two doses (200 mg per kg and 100 mg per kg) of the extract were evaluated for trypanocidal activ

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22

Bollini, Mariela, Ana M. Bruno, María E. Niño, et al. "Synthesis, 2D-QSAR Studies and Biological Evaluation of Quinazoline Derivatives as Potent Anti-Trypanosoma cruzi Agents." Medicinal Chemistry 15, no. 3 (2019): 265–76. http://dx.doi.org/10.2174/1573406414666181005145042.

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Background: Chagas disease affects about 7 million people worldwide. Only two drugs are currently available for the treatment for this parasite disease, namely, benznidazol (Bzn) and nifurtimox (Nfx). Both drugs have limited curative power in the chronic phase of the disease. Therefore, continuous research is an urgent need so as to discover novel therapeutic alternatives. Objective: The development of safer and more efficient therapeutic anti-T. cruzi drugs continues to be a major goal in trypanocidal chemotherapy. Method: Synthesis, 2D-QSAR and drug-like physicochemical properties of a set o

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23

Jardim, Guilherme A. M., Ícaro A. O. Bozzi, Willian X. C. Oliveira, et al. "Copper complexes and carbon nanotube–copper ferrite-catalyzed benzenoid A-ring selenation of quinones: an efficient method for the synthesis of trypanocidal agents." New Journal of Chemistry 43, no. 35 (2019): 13751–63. http://dx.doi.org/10.1039/c9nj02026h.

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A-ring selenation of naphthoquinones and anthraquinones is reported. The reaction proceeds in the presence of a copper source, and provides an efficient and general method for preparing selenium-based quinones with trypanocidal activity.

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24

Pardali, Vasiliki, Erofili Giannakopoulou, Dimitrios-Ilias Balourdas, et al. "Lipophilic Guanylhydrazone Analogues as Promising Trypanocidal Agents: An Extended SAR Study." Current Pharmaceutical Design 26, no. 8 (2020): 838–66. http://dx.doi.org/10.2174/1381612826666200210150127.

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In this report, we extend the SAR analysis of a number of lipophilic guanylhydrazone analogues with respect to in vitro growth inhibition of Trypanosoma brucei and Trypanosoma cruzi. Sleeping sickness and Chagas disease, caused by the tropical parasites T. brucei and T. cruzi, constitute a significant socioeconomic burden in low-income countries of sub-Saharan Africa and Latin America, respectively. Drug development is underfunded. Moreover, current treatments are outdated and difficult to administer, while drug resistance is an emerging concern. The synthesis of adamantane-based compounds tha

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Defaux, Julien, Marta Sala, Xavier Formosa, et al. "Huprines as a new family of dual acting trypanocidal–antiplasmodial agents." Bioorganic & Medicinal Chemistry 19, no. 5 (2011): 1702–7. http://dx.doi.org/10.1016/j.bmc.2011.01.028.

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26

Coro, Julieta, Richard Atherton, Susan Little, et al. "Alkyl-linked bis-THTT derivatives as potent in vitro trypanocidal agents." Bioorganic & Medicinal Chemistry Letters 16, no. 5 (2006): 1312–15. http://dx.doi.org/10.1016/j.bmcl.2005.11.060.

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27

Kelly, John M., Guenter Quack, and Michael M. Miles. "In Vitro and In Vivo Activities of Aminoadamantane and Aminoalkylcyclohexane Derivatives against Trypanosoma brucei." Antimicrobial Agents and Chemotherapy 45, no. 5 (2001): 1360–66. http://dx.doi.org/10.1128/aac.45.5.1360-1366.2001.

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ABSTRACT We reported recently that the bloodstream form of the African trypanosome, Trypanosoma brucei, is sensitive to the anti-influenza virus drug rimantadine. In the present report we describe the trypanocidal properties of a further 62 aminoadamantane and aminoalkylcyclohexane derivatives. Seventeen of the compounds were found to be more active than rimantadine, with four inhibiting growth in vitro of T. brucei by >90% at concentrations of 1 μM. The most active derivative (1-adamantyl-4-amino-cyclohexane) was about 20 to 25 times more effective than rimantadine. We observed a correlati

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28

Jones, Amy J., Marcel Kaiser, and Vicky M. Avery. "Identification and Characterization of FTY720 for the Treatment of Human African Trypanosomiasis." Antimicrobial Agents and Chemotherapy 60, no. 3 (2015): 1859–61. http://dx.doi.org/10.1128/aac.02116-15.

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The screening of a focused library identified FTY720 (Fingolimod; Gilenya) as a potent selective antitrypanosomal compound active againstTrypanosoma brucei gambienseandT. brucei rhodesiense, the causative agents of human African trypanosomiasis (HAT). This is the first report of trypanocidal activity for FTY720, an oral drug registered for the treatment of relapsing multiple sclerosis, and the characterization of sphingolipids as a potential new class of compounds for HAT.

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29

Kajal, Anu, Suman Bala, Neha Sharma, Sunil Kamboj, and Vipin Saini. "Therapeutic Potential of Hydrazones as Anti-Inflammatory Agents." International Journal of Medicinal Chemistry 2014 (March 4, 2014): 1–11. http://dx.doi.org/10.1155/2014/761030.

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Hydrazones are a special class of organic compounds in the Schiff base family. Hydrazones constitute a versatile compound of organic class having basic structure (R1R2C=NNR3R4). The active centers of hydrazone, that is, carbon and nitrogen, are mainly responsible for the physical and chemical properties of the hydrazones and, due to the reactivity toward electrophiles and nucleophiles, hydrazones are used for the synthesis of organic compound such as heterocyclic compounds with a variety of biological activities. Hydrazones and their derivatives are known to exhibit a wide range of interesting

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30

Salgado, Francisco, Mauricio Moncada-Basualto, Josue Pozo-Martinez, et al. "Chemical and biological analysis of 4-acyloxy-3-nitrocoumarins as trypanocidal agents." Arabian Journal of Chemistry 14, no. 3 (2021): 102975. http://dx.doi.org/10.1016/j.arabjc.2020.102975.

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31

Mendonca-Previato, Lucia. "The trans-Sialidase from Trypanosoma cruzi a Putative Target for Trypanocidal Agents." Open Parasitology Journal 4, no. 1 (2010): 111–15. http://dx.doi.org/10.2174/1874421401004010111.

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32

Granero, Gladys E., Maria M. de Bertorello, and Margarita C. Brinon. "ChemInform Abstract: Synthesis of New Isoxazolylnaphthoquinones as Potential Trypanocidal and Antibacterial Agents." ChemInform 30, no. 31 (2010): no. http://dx.doi.org/10.1002/chin.199931155.

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33

Moraes, Francisco Cezar Aquino de, Maria Eduarda Cavalcanti Souza, Lucca Dal Moro, et al. "Prevention of congenital chagas disease by trypanocide treatment in women of reproductive age: A meta-analysis of observational studies." PLOS Neglected Tropical Diseases 18, no. 9 (2024): e0012407. http://dx.doi.org/10.1371/journal.pntd.0012407.

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Background Maternal-foetal transmission of Chagas disease (CD) affects newborns worldwide. Although Benznidazole and Nifurtimox therapies are the standard treatments, their use during pregnancy is contra-indicated. The effectiveness of trypanocidal medications in preventing congenital Chagas Disease (cCD) in the offsprings of women diagnosed with CD was highly suggested by other studies. Methods We performed a systematic review and meta-analysis of studies evaluating the effectiveness of treatment for CD in women of childbearing age and reporting frequencies of cCD in their children. PubMed, S

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Krstin, Sonja, Herbenya Silva Peixoto, and Michael Wink. "Combinations of Alkaloids Affecting Different Molecular Targets with the Saponin Digitonin Can Synergistically Enhance Trypanocidal Activity against Trypanosoma brucei brucei." Antimicrobial Agents and Chemotherapy 59, no. 11 (2015): 7011–17. http://dx.doi.org/10.1128/aac.01315-15.

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ABSTRACTThe flagellateTrypanosoma bruceicauses sleeping sickness in humans and nagana in animals. Only a few drugs are registered to treat trypanosomiasis, but those drugs show severe side effects. Also, because some pathogen strains have become resistant, new strategies are urgently needed to combat this parasitic disease. An underexplored possibility is the application of combinations of several trypanocidal agents, which may potentiate their trypanocidal activity in a synergistic fashion. In this study, the potential synergism of mutual combinations of bioactive alkaloids and alkaloids with

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35

Sülsen, Valeria P., Fernanda M. Frank, Silvia I. Cazorla, et al. "Trypanocidal and Leishmanicidal Activities of Sesquiterpene Lactones from Ambrosia tenuifolia Sprengel (Asteraceae)." Antimicrobial Agents and Chemotherapy 52, no. 7 (2008): 2415–19. http://dx.doi.org/10.1128/aac.01630-07.

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ABSTRACT Bioassay-guided fractionation of the organic extract of Ambrosia tenuifolia Sprengel (Asteraceae) led to the isolation of two bioactive sesquiterpene lactones with significant trypanocidal and leishmanicidal activities. By spectroscopic methods (1H- and 13C-nuclear magnetic resonance, distortionless enhancement by polarization transfer, correlated spectroscopy, heteronuclear multiple-quantum coherence, electron impact-mass spectrometry, and infrared spectroscopy), these compounds were identified as psilostachyin and peruvin. Both compounds showed a marked in vitro trypanocidal activit

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36

Vázquez-Jiménez, Lenci K., Alfredo Juárez-Saldivar, Rogelio Gómez-Escobedo, et al. "Ligand-Based Virtual Screening and Molecular Docking of Benzimidazoles as Potential Inhibitors of Triosephosphate Isomerase Identified New Trypanocidal Agents." International Journal of Molecular Sciences 23, no. 17 (2022): 10047. http://dx.doi.org/10.3390/ijms231710047.

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Trypanosoma cruzi (T. cruzi) is a parasite that affects humans and other mammals. T. cruzi depends on glycolysis as a source of adenosine triphosphate (ATP) supply, and triosephosphate isomerase (TIM) plays a key role in this metabolic pathway. This enzyme is an attractive target for the design of new trypanocidal drugs. In this study, a ligand-based virtual screening (LBVS) from the ZINC15 database using benzimidazole as a scaffold was accomplished. Later, a molecular docking on the interface of T. cruzi TIM (TcTIM) was performed and the compounds were grouped by interaction profiles. Subsequ

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37

Santos-Cruz, Luis Felipe, Bertha Guadalupe Ramírez-Cruz, Miguel García-Salomé, et al. "Genotoxicity assessment of four novel quinazoline-derived trypanocidal agents in the Drosophila wing somatic mutation and recombination test." Mutagenesis 35, no. 4 (2019): 299–310. http://dx.doi.org/10.1093/mutage/gez042.

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Abstract Chagas disease, caused by the protozoan Trypanosoma cruzi, has increased in the world due to migration, travelling and climate change; at present, the principal problem is that common trypanocidal agents have resulted in toxic or inconvenient side effects. We tested for genotoxicity in the standard (ST) and high bioactivation (HB) crosses of Drosophila wing somatic mutation and recombination test, four novel trypanocidal agents derived from 2, 4, 6-triaminquinazoline (TAQ): 2,4-diamino-6 nitro-1,3 diazonaftalene (S-1QN2-1), 2,4-diacetamino-6-amino 1,3 diazonaftalene (D-1), N6-(4,metho

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Pelozo, Mônica Fraccarolli, Giovanna Fiori Serpa Lima, Cleydson Finotti Cordeiro, et al. "Synthesis of New Hybrid Derivatives from Metronidazole and Eugenol Analogues as Trypanocidal Agents." Journal of Pharmacy & Pharmaceutical Sciences 24 (August 16, 2021): 421–34. http://dx.doi.org/10.18433/jpps31839.

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Background: The search for new drug compounds is always challenging and there are several different strategies that involve the most varied and creative approaches in medicinal chemistry. One of them is the technique of molecular hybridisation: forming a hybrid compound from two or more pharmacophoric subunits. These hybrids may maintain the characteristics of the original compound and preferably show improvements to its pharmacological action, with reduced side effects and lower toxicity when compared to the original components. This study specifically focuses on synthesising hybrid molecules

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Shyam, Krishnamurthy, Philip G. Penketh, Alan A. Divo, Regina H. Loomis, Curtis L. Patton, and Alan C. Sartorelli. "Synthesis and evaluation of 1,2,2-tris(sulfonyl)hydrazines as antineoplastic and trypanocidal agents." Journal of Medicinal Chemistry 33, no. 8 (1990): 2259–64. http://dx.doi.org/10.1021/jm00170a033.

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40

López-Muñoz, Marisol, Jessica Johanna Gomez-Peña, Luz Amalia Ríos-Vásquez, et al. "Novel fluorinated quaternary ammonium salts and their in vitro activity as trypanocidal agents." Medicinal Chemistry Research 28, no. 3 (2019): 300–319. http://dx.doi.org/10.1007/s00044-018-02285-2.

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Espinoza-Hicks, José C., Karla Fabiola Chacón-Vargas, Jessica L. Hernández-Rivera, et al. "Novel prenyloxy chalcones as potential leishmanicidal and trypanocidal agents: Design, synthesis and evaluation." European Journal of Medicinal Chemistry 167 (April 2019): 402–13. http://dx.doi.org/10.1016/j.ejmech.2019.02.028.

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42

Pozo-Martínez, Josué, Vicente J. Arán, Matías Zúñiga-Bustos, et al. "In Vitro Evaluation of New 5-Nitroindazolin-3-one Derivatives as Promising Agents against Trypanosoma cruzi." International Journal of Molecular Sciences 25, no. 20 (2024): 11107. http://dx.doi.org/10.3390/ijms252011107.

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Chagas disease is a prevalent health problem in Latin America which has received insufficient attention worldwide. Current treatments for this disease, benznidazole and nifurtimox, have limited efficacy and may cause side effects. A recent study proposed investigating a wide range of nitroindazole and indazolone derivatives as feasible treatments. Therefore, it is proposed that adding a nitro group at the 5-position of the indazole and indazolone structure could enhance trypanocidal activity by inducing oxidative stress through activation of the nitro group by NTRs (nitroreductases). The study

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Kryshchyshyn, Anna, Danylo Kaminskyy, Igor Nektegayev, Philippe Grellier, and Roman Lesyk. "Isothiochromenothiazoles—A Class of Fused Thiazolidinone Derivatives with Established Anticancer Activity That Inhibits Growth of Trypanosoma brucei brucei." Scientia Pharmaceutica 86, no. 4 (2018): 47. http://dx.doi.org/10.3390/scipharm86040047.

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Recently, thiazolidinone derivatives have been widely studied as antiparasitic agents. Previous investigations showed that fused 4-thiazolidinone derivatives (especially thiopyranothiazoles) retain pharmacological activity of their synthetic precursors—simple 5-ene-4-thiazolidinones. A series of isothiochromeno[4a,4-d][1,3] thiazoles was investigated in an in vitro assay towards bloodstream forms of Trypanosoma brucei brucei. All compounds inhibited parasite growth at concentrations in the micromolar range. The established low acute toxicity of this class of compounds along with a good trypano

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Major, Louise L., and Terry K. Smith. "Screening the MayBridge Rule of 3 Fragment Library for Compounds That Interact with the Trypanosoma brucei myo-Inositol-3-Phosphate Synthase and/or Show Trypanocidal Activity." Molecular Biology International 2011 (May 17, 2011): 1–14. http://dx.doi.org/10.4061/2011/389364.

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Inositol-3-phosphate synthase (INO1) has previously been genetically validated as a drug target against Trypanosoma brucei, the causative agent of African sleeping sickness. Chemical intervention of this essential enzyme could lead to new therapeutic agents. Unfortunately, no potent inhibitors of INO1 from any organism have been reported, so a screen for potential novel inhibitors of T. brucei INO1was undertaken. Detection of inhibition of T. brucei INO1 is problematic due to the nature of the reaction. Direct detection requires differentiation between glucose-6-phosphate and inositol-3-phosph

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Morty, Rory E., Linda Troeberg, Robert N. Pike, et al. "A trypanosome oligopeptidase as a target for the trypanocidal agents pentamidine, diminazene and suramin." FEBS Letters 433, no. 3 (1998): 251–56. http://dx.doi.org/10.1016/s0014-5793(98)00914-4.

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Scarim, Cauê, Francisco Olmo, Elizabeth Ferreira, Chung Chin, John Kelly, and Amanda Francisco. "Image-Based In Vitro Screening Reveals the Trypanostatic Activity of Hydroxymethylnitrofurazone against Trypanosoma cruzi." International Journal of Molecular Sciences 22, no. 13 (2021): 6930. http://dx.doi.org/10.3390/ijms22136930.

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Hydroxymethylnitrofurazone (NFOH) is a therapeutic candidate for Chagas disease (CD). It has negligible hepatotoxicity in a murine model compared to the front-line drug benznidazole (BZN). Here, using Trypanosoma cruzi strains that express bioluminescent and/or fluorescent reporter proteins, we further investigated the in vitro and in vivo activity of NFOH to define whether the compound is trypanocidal or trypanostatic. The in vitro activity was assessed by exploiting the fluorescent reporter strain using wash-out assays and real-time microscopy. For animal experimentation, BALB/c mice were in

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Gaona-López, Carlos, Domingo Méndez-Álvarez, Alonzo Gonzalez-Gonzalez, et al. "In Silico Investigation of TATA-Binding Protein as a Therapeutic Target for Chagas Disease: Insights into FDA Drug Repositioning." Pharmaceuticals 18, no. 6 (2025): 845. https://doi.org/10.3390/ph18060845.

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Background: Parasitic diseases, particularly Chagas disease caused by Trypanosoma cruzi, primarily affect developing countries but are now spreading to wealthier nations due to changing migration patterns. With approximately 8 to 9 million cases annually and a rise in drug resistance and side effects, there is an urgent need for new therapeutic approaches. Objectives: This study aimed to identify potential pharmacological compounds to target the TATA Binding Protein (TBP) of T. cruzi. Methods: Over eleven thousand FDA-approved pharmacological compounds were analyzed using in silico methods, in

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Elso, Orlando G., Augusto E. Bivona, Andrés Sanchez Alberti, et al. "Trypanocidal Activity of Four Sesquiterpene Lactones Isolated from Asteraceae Species." Molecules 25, no. 9 (2020): 2014. http://dx.doi.org/10.3390/molecules25092014.

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The sesquiterpene lactones eupatoriopicrin, estafietin, eupahakonenin B and minimolide have been isolated from Argentinean Astearaceae species and have been found to be active against Trypanosoma cruzi epimastigotes. The aim of this work was to evaluate the activity of these compounds by analyzing their effect against the stages of the parasites that are infective for the human. Even more interesting, we aimed to determine the effect of the most active and selective compound on an in vivo model of T. cruzi infection. Eupatoriopicrin was the most active against amastigotes and tripomastigotes (

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Sippel, H., U. Steinmann, and C. J. Estler. "Influence of Pentamidine and Two New Trypanocidal Agents (DAPI, DIPI) on Liver Metabolism of Mice." Pharmacology & Toxicology 69, no. 5 (1991): 372–77. http://dx.doi.org/10.1111/j.1600-0773.1991.tb01314.x.

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Atsriku, C., D. G. Watson, M. H. Grant, and G. G. Skellern. "The effect of inducing agents on the metabolism of trypanocidal diamidines by isolated rat hepatocytes." Chemico-Biological Interactions 146, no. 3 (2003): 297–305. http://dx.doi.org/10.1016/j.cbi.2003.09.005.

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