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1

Steverding, Dietmar, and Kevin M. Tyler. "Novel antitrypanosomal agents." Expert Opinion on Investigational Drugs 14, no. 8 (2005): 939–55. http://dx.doi.org/10.1517/13543784.14.8.939.

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2

Issa, Victor Sarli, and Edimar Alcides Bocchi. "Antitrypanosomal agents: treatment or threat?" Lancet 376, no. 9743 (2010): 768. http://dx.doi.org/10.1016/s0140-6736(10)61372-4.

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3

Schmidt, Ines, Sarah Göllner, Antje Fuß, et al. "Bistacrines as potential antitrypanosomal agents." Bioorganic & Medicinal Chemistry 25, no. 16 (2017): 4526–31. http://dx.doi.org/10.1016/j.bmc.2017.06.051.

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4

Ryczak, Jasmin, Ma'ayan Papini, Annette Lader, et al. "2-Arylpaullones are selective antitrypanosomal agents." European Journal of Medicinal Chemistry 64 (June 2013): 396–400. http://dx.doi.org/10.1016/j.ejmech.2013.03.065.

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5

Rassi, Anis, Anis Rassi, and José Antonio Marin-Neto. "Antitrypanosomal agents: treatment or threat? – Authors' reply." Lancet 376, no. 9743 (2010): 768–69. http://dx.doi.org/10.1016/s0140-6736(10)61373-6.

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6

Silva, Daniel G., J. Robert Gillespie, Ranae M. Ranade, et al. "New Class of Antitrypanosomal Agents Based on Imidazopyridines." ACS Medicinal Chemistry Letters 8, no. 7 (2017): 766–70. http://dx.doi.org/10.1021/acsmedchemlett.7b00202.

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7

Ding, Dazhong, Yaxue Zhao, Qingqing Meng, et al. "Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents." ACS Medicinal Chemistry Letters 1, no. 4 (2010): 165–69. http://dx.doi.org/10.1021/ml100013s.

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8

Rodríguez Arce, Esteban, Eugenia Putzu, Michel Lapier, et al. "New heterobimetallic ferrocenyl derivatives are promising antitrypanosomal agents." Dalton Transactions 48, no. 22 (2019): 7644–58. http://dx.doi.org/10.1039/c9dt01317b.

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9

Qiao, Zhitao, Qi Wang, Fenglong Zhang, et al. "Chalcone–Benzoxaborole Hybrid Molecules as Potent Antitrypanosomal Agents." Journal of Medicinal Chemistry 55, no. 7 (2012): 3553–57. http://dx.doi.org/10.1021/jm2012408.

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10

Papadopoulou, Maria V., William D. Bloomer, Howard S. Rosenzweig, Ivan P. O'Shea, Shane R. Wilkinson, and Marcel Kaiser. "3-Nitrotriazole-based piperazides as potent antitrypanosomal agents." European Journal of Medicinal Chemistry 103 (October 2015): 325–34. http://dx.doi.org/10.1016/j.ejmech.2015.08.042.

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11

Cogo, Juliana, Juan Cantizani, Ignacio Cotillo, et al. "Quinoxaline derivatives as potential antitrypanosomal and antileishmanial agents." Bioorganic & Medicinal Chemistry 26, no. 14 (2018): 4065–72. http://dx.doi.org/10.1016/j.bmc.2018.06.033.

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12

Veale, Clinton G. L., Dustin Laming, Tarryn Swart, Kelly Chibale, and Heinrich C. Hoppe. "Exploring the Antiplasmodial 2‐Aminopyridines as Potential Antitrypanosomal Agents." ChemMedChem 14, no. 24 (2019): 2034–41. http://dx.doi.org/10.1002/cmdc.201900492.

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13

Kryshchyshyn, Anna, Danylo Kaminskyy, Oleksandr Karpenko, Andrzej Gzella, Philippe Grellier, and Roman Lesyk. "Thiazolidinone/thiazole based hybrids – New class of antitrypanosomal agents." European Journal of Medicinal Chemistry 174 (July 2019): 292–308. http://dx.doi.org/10.1016/j.ejmech.2019.04.052.

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14

Kryshchyshyn, Anna, Danylo Kaminskyy, Philippe Grellier, and Roman Lesyk. "Trends in research of antitrypanosomal agents among synthetic heterocycles." European Journal of Medicinal Chemistry 85 (October 2014): 51–64. http://dx.doi.org/10.1016/j.ejmech.2014.07.092.

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15

Belmonte-Reche, Efres, Marta Martínez-García, Pablo Peñalver, et al. "Tyrosol and hydroxytyrosol derivatives as antitrypanosomal and antileishmanial agents." European Journal of Medicinal Chemistry 119 (August 2016): 132–40. http://dx.doi.org/10.1016/j.ejmech.2016.04.047.

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16

Sealey-Cardona, Marco, Simon Cammerer, Simon Jones, et al. "Kinetic Characterization of Squalene Synthase from Trypanosoma cruzi: Selective Inhibition by Quinuclidine Derivatives." Antimicrobial Agents and Chemotherapy 51, no. 6 (2007): 2123–29. http://dx.doi.org/10.1128/aac.01454-06.

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ABSTRACT The biosynthesis of sterols is a major route for the development of antitrypanosomals. Squalene synthase (SQS) catalyzes the first step committed to the biosynthesis of sterols within the isoprenoid pathway, and several inhibitors of the enzyme have selective antitrypanosomal activity both in vivo and in vitro. The enzyme from Trypanosoma cruzi is a 404-amino-acid protein with a clearly identifiable membrane-spanning region. In an effort to generate soluble recombinant enzyme, we have expressed in Escherichia coli several truncated versions of T. cruzi SQS with a His tag attached to t
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17

Tullius Scotti, Marcus, Luciana Scotti, Hamilton Ishiki, et al. "Natural Products as a Source for Antileishmanial and Antitrypanosomal Agents." Combinatorial Chemistry & High Throughput Screening 19, no. 7 (2016): 537–53. http://dx.doi.org/10.2174/1386207319666160506123921.

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18

Kryshchyshyn, Anna, Danylo Kaminskyy, Philippe Grellier, and Roman Lesyk. "ChemInform Abstract: Trends in Research of Antitrypanosomal Agents Among Synthetic Heterocycles." ChemInform 45, no. 45 (2014): no. http://dx.doi.org/10.1002/chin.201445286.

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19

Chianese, Giuseppina, Ernesto Fattorusso, Fernando Scala, et al. "Manadoperoxides, a new class of potent antitrypanosomal agents of marine origin." Organic & Biomolecular Chemistry 10, no. 35 (2012): 7197. http://dx.doi.org/10.1039/c2ob26124c.

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20

Papadopoulou, Maria V., William D. Bloomer, Howard S. Rosenzweig, Shane R. Wilkinson, and Marcel Kaiser. "Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents." European Journal of Medicinal Chemistry 87 (November 2014): 79–88. http://dx.doi.org/10.1016/j.ejmech.2014.09.045.

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21

Romero, Angel H., Jonathan Rodríguez, Yael García-Marchan, Jacques Leañez, Xenón Serrano-Martín, and Simón E. López. "Aryl- or heteroaryl-based hydrazinylphthalazine derivatives as new potential antitrypanosomal agents." Bioorganic Chemistry 72 (June 2017): 51–56. http://dx.doi.org/10.1016/j.bioorg.2017.03.008.

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22

Benítez, Julio, Aline Cavalcanti de Queiroz, Isabel Correia, et al. "New oxidovanadium(IV) N -acylhydrazone complexes: Promising antileishmanial and antitrypanosomal agents." European Journal of Medicinal Chemistry 62 (April 2013): 20–27. http://dx.doi.org/10.1016/j.ejmech.2012.12.036.

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23

Ettari, Roberta, Santo Previti, Sandro Cosconati, et al. "Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents." Bioorganic & Medicinal Chemistry Letters 26, no. 15 (2016): 3453–56. http://dx.doi.org/10.1016/j.bmcl.2016.06.047.

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24

Gamaleldin, Noha M., Walid Bakeer, Ahmed M. Sayed, et al. "Exploration of Chemical Diversity and Antitrypanosomal Activity of Some Red Sea-Derived Actinomycetes Using the OSMAC Approach Supported by LC-MS-Based Metabolomics and Molecular Modelling." Antibiotics 9, no. 9 (2020): 629. http://dx.doi.org/10.3390/antibiotics9090629.

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In the present study, we investigated the actinomycetes associated with the Red Sea-derived soft coral Sarcophyton glaucum in terms of biological and chemical diversity. Three strains were cultivated and identified to be members of genera Micromonospora, Streptomyces, and Nocardiopsis; out of them, Micromonospora sp. UR17 was putatively characterized as a new species. In order to explore the chemical diversity of these actinobacteria as far as possible, they were subjected to a series of fermentation experiments under altering conditions, that is, solid and liquid fermentation along with co-fe
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25

Okaiyeto, Kunle, and Anthony I. Okoh. "In Vitro Assessment of Antiplasmodial and Antitrypanosomal Activities of Chloroform, Ethyl Acetate and Ethanol Leaf Extracts of Oedera genistifolia." Applied Sciences 10, no. 19 (2020): 6987. http://dx.doi.org/10.3390/app10196987.

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The high resistance evolution of protozoans to the existing antiparasitic drugs has necessitated the quest for novel and effective drugs against plasmodium and trypanosome parasites. As a result, this study aimed to assess the antiplasmodial and antitrypanosomal potentials of chloroform, ethyl acetate and ethanol leaf extracts of Oedera genistifolia. Standard biochemical procedures were explored for the plant extraction and gas chromatography-mass spectroscopy (GCMS) was used to identify the bioactive compounds in the crude extracts. The cytotoxic effects of the crude extracts were assessed ag
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26

Augustyns, K., K. Amssoms, A. Yamani, P. Rajan, and A. Haemers. "Trypanothione as a Target in the Design of Antitrypanosomal and Antileishmanial Agents." Current Pharmaceutical Design 7, no. 12 (2001): 1117–41. http://dx.doi.org/10.2174/1381612013397564.

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27

Figgitt, D., W. Denny, P. Chavalitshewinkoon, P. Wilairat, and R. Ralph. "In vitro study of anticancer acridines as potential antitrypanosomal and antimalarial agents." Antimicrobial Agents and Chemotherapy 36, no. 8 (1992): 1644–47. http://dx.doi.org/10.1128/aac.36.8.1644.

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28

Kosower, EM, AE Radkowsky, AH Fairlamb, SL Croft, and RA Neal. "Bimane cyclic esters, possible stereologues of trypanothione as antitrypanosomal agents. Bimanes 29." European Journal of Medicinal Chemistry 30, no. 9 (1995): 659–71. http://dx.doi.org/10.1016/0223-5234(96)88283-3.

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29

Hernandes, Marcelo Zaldini, Marcelo Montenegro Rabello, Ana Cristina Lima Leite, et al. "Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents." Bioorganic & Medicinal Chemistry 18, no. 22 (2010): 7826–35. http://dx.doi.org/10.1016/j.bmc.2010.09.056.

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30

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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31

Wang, Jiayi, Marcel Kaiser, and Brent Copp. "Investigation of Indolglyoxamide and Indolacetamide Analogues of Polyamines as Antimalarial and Antitrypanosomal Agents." Marine Drugs 12, no. 6 (2014): 3138–60. http://dx.doi.org/10.3390/md12063138.

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32

Scalese, Gonzalo, Ignacio Machado, Isabel Correia, et al. "Exploring oxidovanadium(iv) homoleptic complexes with 8-hydroxyquinoline derivatives as prospective antitrypanosomal agents." New Journal of Chemistry 43, no. 45 (2019): 17756–73. http://dx.doi.org/10.1039/c9nj02589h.

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[V<sup>IV</sup>O(L-H)<sub>2</sub>] and [V<sup>V</sup>O(OCH<sub>3</sub>)(L-H)<sub>2</sub>] compounds of 8-hydroxyquinoline derivatives L showed activity against Trypanosoma cruzi and Leishmania infantum and high selectivities. Metallomics and interaction with BSA, apo-HTF and DNA were studied.
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33

Turner, William R., and Leslie M. Werbel. "Novel bis[1,6-dihydro-6,6-dimethyl-1,3,5-triazine-2,4-diamines] as antitrypanosomal agents." Journal of Medicinal Chemistry 28, no. 11 (1985): 1728–40. http://dx.doi.org/10.1021/jm00149a032.

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34

Chanquia, Santiago N., Facundo Larregui, Vanesa Puente, Carlos Labriola, Elisa Lombardo, and Guadalupe García Liñares. "Synthesis and biological evaluation of new quinoline derivatives as antileishmanial and antitrypanosomal agents." Bioorganic Chemistry 83 (March 2019): 526–34. http://dx.doi.org/10.1016/j.bioorg.2018.10.053.

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35

Carvalho, Samir A., Larisse O. Feitosa, Márcio Soares, et al. "Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents." European Journal of Medicinal Chemistry 54 (August 2012): 512–21. http://dx.doi.org/10.1016/j.ejmech.2012.05.041.

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36

Papadopoulou, Maria V., William D. Bloomer, Howard S. Rosenzweig, et al. "Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation." Bioorganic & Medicinal Chemistry 23, no. 19 (2015): 6467–76. http://dx.doi.org/10.1016/j.bmc.2015.08.014.

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37

Cunha, André Barreto, Ronan Batista, María Ángeles Castro, and Jorge Mauricio David. "Chemical Strategies towards the Synthesis of Betulinic Acid and Its More Potent Antiprotozoal Analogues." Molecules 26, no. 4 (2021): 1081. http://dx.doi.org/10.3390/molecules26041081.

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Betulinic acid (BA, 3β-hydroxy-lup-20(29)-en-28-oic acid) is a pentacyclic triterpene acid present predominantly in Betula ssp. (Betulaceae) and is also widely spread in many species belonging to different plant families. BA presents a wide spectrum of remarkable pharmacological properties, such as cytotoxic, anti-HIV, anti-inflammatory, antidiabetic and antimicrobial activities, including antiprotozoal effects. The present review first describes the sources of BA and discusses the chemical strategies to produce this molecule starting from betulin, its natural precursor. Next, the antiprotozoa
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38

Flittner, Dagmar, Marcel Kaiser, Pascal Mäser, Norberto P. Lopes, and Thomas J. Schmidt. "The Alkaloid-Enriched Fraction of Pachysandra terminalis (Buxaceae) Shows Prominent Activity against Trypanosoma brucei rhodesiense." Molecules 26, no. 3 (2021): 591. http://dx.doi.org/10.3390/molecules26030591.

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In the course of our studies on antiprotozoal natural products and following our recent discovery that certain aminosteroids and aminocycloartanoid compounds from Holarrhena africana A. DC. (Apocynaceae) and Buxus sempervirens L. (Buxaceae), respectively, are strong and selective antitrypanosomal agents, we have extended these studies to another plant, related to the latter—namely, Pachysandra terminalis Sieb. and Zucc. (Buxaceae). This species is known to contain aminosteroids similar to those of Holarrhena and structurally related to the aminocycloartanoids of Buxus. The dicholoromethane ext
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39

Twumasi, Emmanuella Bema, Pearl Ihuoma Akazue, Kwaku Kyeremeh, et al. "Antischistosomal, antionchocercal and antitrypanosomal potentials of some Ghanaian traditional medicines and their constituents." PLOS Neglected Tropical Diseases 14, no. 12 (2020): e0008919. http://dx.doi.org/10.1371/journal.pntd.0008919.

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Background Ghana is endemic for some neglected tropical diseases (NTDs) including schistosomiasis, onchocerciasis and lymphatic filariasis. The major intervention for these diseases is mass drug administration of a few repeatedly recycled drugs which is a cause for major concern due to reduced efficacy of the drugs and the emergence of drug resistance. Evidently, new treatments are needed urgently. Medicinal plants, on the other hand, have a reputable history as important sources of potent therapeutic agents in the treatment of various diseases among African populations, Ghana inclusively, and
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40

Walzer, P. D., C. K. Kim, J. Foy, M. J. Linke, and M. T. Cushion. "Cationic antitrypanosomal and other antimicrobial agents in the therapy of experimental Pneumocystis carinii pneumonia." Antimicrobial Agents and Chemotherapy 32, no. 6 (1988): 896–905. http://dx.doi.org/10.1128/aac.32.6.896.

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41

KOSOWER, E. M., A. E. RADKOWSKY, A. H. FAIRLAMB, S. L. CROFT, and R. A. NEAL. "ChemInform Abstract: Bimane Cyclic Esters, Possible Stereologues of Trypanothione as Antitrypanosomal Agents. Bimanes 29." ChemInform 27, no. 2 (2010): no. http://dx.doi.org/10.1002/chin.199602197.

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42

Ding, Dazhong, Qingqing Meng, Guangwei Gao, et al. "Design, Synthesis, and Structure−Activity Relationship ofTrypanosoma bruceiLeucyl-tRNA Synthetase Inhibitors as Antitrypanosomal Agents." Journal of Medicinal Chemistry 54, no. 5 (2011): 1276–87. http://dx.doi.org/10.1021/jm101225g.

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43

Papadopoulou, Maria V., William D. Bloomer, Howard S. Rosenzweig, et al. "Novel 3-Nitro-1H-1,2,4-triazole-Based Amides and Sulfonamides as Potential Antitrypanosomal Agents." Journal of Medicinal Chemistry 55, no. 11 (2012): 5554–65. http://dx.doi.org/10.1021/jm300508n.

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44

Jadav, Surender S., Vishnu N. Badavath, Ramesh Ganesan, Narayana M. Ganta, Dominique Besson, and Venkatesan Jayaprakash. "Biological Evaluation of 2-aminothiazole Hybrid as Antimalarial and Antitrypanosomal Agents: Design and Synthesis." Anti-Infective Agents 18, no. 2 (2020): 101–8. http://dx.doi.org/10.2174/2211352516666181016122537.

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Background: A series of 2-aminothiazole schiff’s bases (1-24) were synthesized and screened against a few neglected tropical disorders (NTDs). Compounds 12 and 14 were found to have antitrypanosidal activity, whereas compound 14 was found to be more effective than standard benznidazole. The antiplasmodial assay provided three specific and effective compounds (9, 12 and 24) than standard chloroquine. Compound (21) inhibited Leishmania infantum, almost similar to Miltefosine. Methods: All the compounds were subjected to cytotoxicity assay and none of the compounds were found to be cytotoxicity.
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45

Valente, Maria, Víctor M. Castillo-Acosta, Antonio E. Vidal, and Dolores González-Pacanowska. "Overview of the role of kinetoplastid surface carbohydrates in infection and host cell invasion: prospects for therapeutic intervention." Parasitology 146, no. 14 (2019): 1743–54. http://dx.doi.org/10.1017/s0031182019001355.

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AbstractKinetoplastid parasites are responsible for serious diseases in humans and livestock such as Chagas disease and sleeping sickness (caused by Trypanosoma cruzi and Trypanosoma brucei, respectively), and the different forms of cutaneous, mucocutaneous and visceral leishmaniasis (produced by Leishmania spp). The limited number of antiparasitic drugs available together with the emergence of resistance underscores the need for new therapeutic agents with novel mechanisms of action. The use of agents binding to surface glycans has been recently suggested as a new approach to antitrypanosomal
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46

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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47

Oluwafemi, Awotunde J., Emmanuel O. Okanla, Pelayo Camps, et al. "Evaluation of Cryptolepine and Huperzine Derivatives as Lead Compounds towards New Agents for the Treatment of Human African Trypanosomiasis." Natural Product Communications 4, no. 2 (2009): 1934578X0900400. http://dx.doi.org/10.1177/1934578x0900400205.

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The alkaloid cryptolepine (1) and eight synthetic analogues (2-8) were assessed for in vitro activities against Trypanosoma brucei. Four of the analogues were found to be highly potent with IC50 values of less than 3 nM and three of these were assessed against T. brucei brucei infection in rats. The most effective compound was 2, 7-dibromocryptolepine (7); a single oral dose of 20 mg/kg suppressed parasitaemia and increased the mean survival time to 13.6 days compared with 8.4 days for untreated controls. In addition, four huperzine derivatives (9-12) were shown to have in vitro antitrypanosom
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48

Cogo, Juliana, Vanessa Kaplum, Diego Pereira Sangi, Tânia Ueda-Nakamura, Arlene Gonçalves Corrêa, and Celso Vataru Nakamura. "Synthesis and biological evaluation of novel 2,3-disubstituted quinoxaline derivatives as antileishmanial and antitrypanosomal agents." European Journal of Medicinal Chemistry 90 (January 2015): 107–23. http://dx.doi.org/10.1016/j.ejmech.2014.11.018.

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49

Fernández, Mariana, Lorena Becco, Isabel Correia, et al. "Oxidovanadium(IV) and dioxidovanadium(V) complexes of tridentate salicylaldehyde semicarbazones: Searching for prospective antitrypanosomal agents." Journal of Inorganic Biochemistry 127 (October 2013): 150–60. http://dx.doi.org/10.1016/j.jinorgbio.2013.02.010.

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50

Larayetan, Rotimi, Zacchaeus S. Ololade, Oluranti O. Ogunmola, and Ayodele Ladokun. "Phytochemical Constituents, Antioxidant, Cytotoxicity, Antimicrobial, Antitrypanosomal, and Antimalarial Potentials of the Crude Extracts of Callistemon citrinus." Evidence-Based Complementary and Alternative Medicine 2019 (August 28, 2019): 1–14. http://dx.doi.org/10.1155/2019/5410923.

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Plants are reservoir for potentially useful bioactive compounds, and owing to the rising occurrences of drug resistance to malaria parasites, there is a need to discover and develop new phytochemicals in plant that can be used as antimalarial agents. In this study, we gave a detailed description of the phytochemicals present in both ethyl acetate and methanolic extracts of Callistemon citrinus (C. citrinus) using Gas Chromatography-Mass Spectrometry (GC-MS) analysis; both extracts were also evaluated for their in vitro antimalarial, antitrypanosomal, and cytotoxicity activities against Trypano
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