Journal articles: 'Antitrypanosomal agents'

1

Steverding, Dietmar, and Kevin M. Tyler. "Novel antitrypanosomal agents." Expert Opinion on Investigational Drugs 14, no. 8 (July 29, 2005): 939–55. http://dx.doi.org/10.1517/13543784.14.8.939.

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

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3

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

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Ryczak, Jasmin, Ma'ayan Papini, Annette Lader, Abedelmajeed Nasereddin, Dmitry Kopelyanskiy, Lutz Preu, Charles L. Jaffe, and Conrad Kunick. "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 (September 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, Zackary M. Herbst, Uyen T. T. Nguyen, Frederick S. Buckner, Carlos A. Montanari, and Michael H. Gelb. "New Class of Antitrypanosomal Agents Based on Imidazopyridines." ACS Medicinal Chemistry Letters 8, no. 7 (June 29, 2017): 766–70. http://dx.doi.org/10.1021/acsmedchemlett.7b00202.

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7

Ding, Dazhong, Yaxue Zhao, Qingqing Meng, Dongsheng Xie, Bakela Nare, Daitao Chen, Cyrus J. Bacchi, et al. "Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents." ACS Medicinal Chemistry Letters 1, no. 4 (April 6, 2010): 165–69. http://dx.doi.org/10.1021/ml100013s.

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8

Rodríguez Arce, Esteban, Eugenia Putzu, Michel Lapier, Juan Diego Maya, Claudio Olea Azar, Gustavo A. Echeverría, Oscar E. Piro, 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, Zhongli Wang, Tana Bowling, Bakela Nare, Robert T. Jacobs, et al. "Chalcone–Benzoxaborole Hybrid Molecules as Potent Antitrypanosomal Agents." Journal of Medicinal Chemistry 55, no. 7 (March 14, 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, Diego Pereira Sangi, Arlene Gonçalves Corrêa, Tânia Ueda-Nakamura, Benedito Prado Dias Filho, José Julio Martín, and Celso Vataru Nakamura. "Quinoxaline derivatives as potential antitrypanosomal and antileishmanial agents." Bioorganic & Medicinal Chemistry 26, no. 14 (August 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 (November 12, 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, Verónica Gómez-Pérez, Ricardo Lucas, Francisco Gamarro, José María Pérez-Victoria, and Juan Carlos Morales. "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, Luis M. Ruiz-Pérez, Reto Brun, Ian H. Gilbert, Julio A. Urbina, and Dolores González-Pacanowska. "Kinetic Characterization of Squalene Synthase from Trypanosoma cruzi: Selective Inhibition by Quinuclidine Derivatives." Antimicrobial Agents and Chemotherapy 51, no. 6 (March 19, 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 the amino terminus. Deletions of both the amino- and carboxyl-terminal regions generated active and soluble forms of the enzyme. The highest levels of soluble protein were achieved when 24 and 36 amino acids were eliminated from the amino and carboxyl regions, respectively, yielding a protein of 41.67 kDa. The Michaelis-Menten constants of the purified enzyme for farnesyl diphosphate and NAD (NADPH) were 5.25 and 23.34 μM, respectively, whereas the V max was 1,428.56 nmol min−1mg−1. Several quinuclidine derivatives with antiprotozoal activity in vitro were found to be selective inhibitors of recombinant T. cruzi SQS in comparative assays with the human enzyme, with 50% inhibitory concentration values in the nanomolar range. These data suggest that selective inhibition of T. cruzi SQS may be an efficient strategy for the development of new antitrypanosomal agents.

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17

Tullius Scotti, Marcus, Luciana Scotti, Hamilton Ishiki, Frederico Fávaro Ribeiro, Rayssa Marques Duarte da Cruz, Michelle Pedrosa de Oliveira, and Francisco Jaime Bezerra Mendonça. "Natural Products as a Source for Antileishmanial and Antitrypanosomal Agents." Combinatorial Chemistry & High Throughput Screening 19, no. 7 (July 12, 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 (October 23, 2014): no. http://dx.doi.org/10.1002/chin.201445286.

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19

Chianese, Giuseppina, Ernesto Fattorusso, Fernando Scala, Roberta Teta, Barbara Calcinai, Giorgio Bavestrello, Henny A. Dien, Marcel Kaiser, Deniz Tasdemir, and Orazio Taglialatela-Scafati. "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, Marina Amaral Alves, Magna S. Alexandre-Moreira, Eliezer J. Barreiro, Lidia Moreira Lima, 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, Santina Maiorana, Tanja Schirmeister, Silvana Grasso, and Maria Zappalà. "Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents." Bioorganic & Medicinal Chemistry Letters 26, no. 15 (August 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, Yara I. Shamikh, Ahmed O. El-Gendy, Hossam M. Hassan, Hannes Horn, Usama Ramadan Abdelmohsen, and Wael N. Hozzein. "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 (September 22, 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-fermentation with a mycolic acid-containing strain, namely Nocardia sp. UR23. Each treatment was found to affect these actinomycetes differently in terms of biological activity (i.e., antitrypanosomal activity) and chemical profiles evidenced by LC-HRES-MS-based metabolomics and multivariate analysis. Thereafter, orthogonal projections to latent structures discriminant analysis (OPLS-DA) suggested a number of metabolites to be associated with the antitrypanosomal activity of the active extracts. The subsequent in silico screenings (neural networking-based and docking-based) further supported the OPLS-DA results and prioritized desferrioxamine B (3), bafilomycin D (10), and bafilomycin A1 (11) as possible antitrypanosomal agents. Our approach in this study can be applied as a primary step in the exploration of bioactive natural products, particularly those from actinomycetes.

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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 (October 7, 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 against human cervix adenocarcinoma (HeLa cells) and their antiparasitic activities were investigated against Plasmodium falciparum strain 3D7 and Trypanosoma brucei brucei. GCMS analyses of the crude extracts revealed the bioactive compounds that could be responsible for the biological activities. The extracts had no cytotoxic effect on HeLa cells and demonstrated good antiplasmodial activity (chloroform extract: IC50 = 11.6 µg∙mL−1, ethyl acetate extract: IC50 = 3.3 µg∙mL−1 and ethanol extract: IC50 = 3.7 µg∙mL−1). Likewise, they showed excellent antitrypanosomal activity with IC50 = 0.5 µg∙mL−1 for chloroform and ethyl acetate extracts and IC50 = 0.4 µg∙mL−1 for the ethanol extract. Findings from the present study indicated that O. genistifolia could be a good source of strong antiplasmodial and antitrypanosomal agents.

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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 (August 1, 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 (August 1, 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 (January 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, Marcos Veríssimo Oliveira Cardoso, Diogo Rodrigo Magalhaes Moreira, Dalci José Brondani, Carlos Alberto Simone, Luiza Campos Reis, Marina Assis Souza, and Valéria Rego Alves Pereira. "Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents." Bioorganic & Medicinal Chemistry 18, no. 22 (November 15, 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 (December 14, 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 (May 28, 2014): 3138–60. http://dx.doi.org/10.3390/md12063138.

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32

Scalese, Gonzalo, Ignacio Machado, Isabel Correia, Joao Costa Pessoa, Lucía Bilbao, Leticia Pérez-Diaz, and Dinorah Gambino. "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^IVO(L-H)₂] and [V^VO(OCH₃)(L-H)₂] 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 (November 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, Thadeu E. M. M. Costa, Maria G. Henriques, Kelly Salomão, Solange L. de Castro, 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, Ivan P. O’Shea, Shane R. Wilkinson, Marcel Kaiser, Eric Chatelain, and Jean-Robert Ioset. "Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation." Bioorganic & Medicinal Chemistry 23, no. 19 (October 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 (February 18, 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 antiprotozoal properties of BA are briefly discussed and the chemical strategies for the synthesis of analogues displaying antiplasmodial, antileishmanial and antitrypanosomal activities are systematically presented. The antiplasmodial activity described for BA was moderate, nevertheless, some C-3 position acylated analogues showed an improvement of this activity and the hybrid models—with artesunic acid—showed the most interesting properties. Some analogues also presented more intense antileishmanial activities compared with BA, and, in addition to these, heterocycles fused to C-2/C-3 positions and amide derivatives were the most promising analogues. Regarding the antitrypanosomal activity, some interesting antitrypanosomal derivatives were prepared by amide formation at the C-28 carboxylic group of the lupane skeleton. Considering that BA can be produced either by isolation of different plant extracts or by chemical transformation of betulin, easily obtained from Betula ssp., it could be said that BA is a molecule of great interest as a starting material for the synthesis of novel antiprotozoal agents.

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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 (January 23, 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 extract obtained from aerial parts of P. terminalis and, in particular, its alkaloid fraction obtained by acid–base partitioning showed prominent activity against Trypanosoma brucei rhodesiense (Tbr). Activity-guided fractionation along with extended UHPLC-(+)ESI QTOF MS analyses coupled with partial least squares (PLS) regression modelling relating the analytical profiles of various fractions with their bioactivity against Tbr highlighted eighteen constituents likely responsible for the antitrypanosomal activity. Detailed analysis of their (+)ESI mass spectral fragmentation allowed identification of four known constituents of P. terminalis as well as structural characterization of ten further amino-/amidosteroids not previously reported from this plant.

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39

Twumasi, Emmanuella Bema, Pearl Ihuoma Akazue, Kwaku Kyeremeh, Theresa Manful Gwira, Jennifer Keiser, Fidelis Cho-Ngwa, Adrian Flint, et al. "Antischistosomal, antionchocercal and antitrypanosomal potentials of some Ghanaian traditional medicines and their constituents." PLOS Neglected Tropical Diseases 14, no. 12 (December 31, 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 provide very useful starting points for the discovery of much-needed new or alternative drugs. Methodology/Principal findings In this study, extracts of fifteen traditional medicines used for treating various NTDs in local communities were screened in vitro for efficacy against schistosomiasis, onchocerciasis and African trypanosomiasis. Two extracts, NTD-B4-DCM and NTD-B7-DCM, prepared from traditional medicines used to treat schistosomiasis, displayed the highest activity (IC50 = 30.5 μg/mL and 30.8 μg/mL, respectively) against Schistosoma mansoni adult worms. NTD-B2-DCM, also obtained from an antischistosomal remedy, was the most active against female and male adult Onchocera ochengi worms (IC50 = 76.2 μg/mL and 76.7 μg/mL, respectively). Antitrypanosomal assay of the extracts against Trypanosoma brucei brucei gave the most promising results (IC50 = 5.63 μg/mL to 18.71 μg/mL). Incidentally, NTD-B4-DCM and NTD-B2-DCM, also exhibited the greatest antitrypanosomal activities (IC50 = 5.63 μg/mL and 7.12 μg/mL, respectively). Following the favourable outcome of the antitrypanosomal screening, this assay was selected for bioactivity-guided fractionation. NTD-B4-DCM, the most active extract, was fractionated and subsequent isolation of bioactive constituents led to an eupatoriochromene-rich oil (42.6%) which was 1.3-fold (IC50 <0.0977 μg/mL) more active than the standard antitrypanosomal drug, diminazene aceturate (IC50 = 0.13 μg/mL). Conclusion/Significance These findings justify the use of traditional medicines and demonstrate their prospects towards NTDs drug discovery.

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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 (June 1, 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 (August 12, 2010): no. http://dx.doi.org/10.1002/chin.199602197.

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42

Ding, Dazhong, Qingqing Meng, Guangwei Gao, Yaxue Zhao, Qing Wang, Bakela Nare, Robert Jacobs, et al. "Design, Synthesis, and Structure−Activity Relationship ofTrypanosoma bruceiLeucyl-tRNA Synthetase Inhibitors as Antitrypanosomal Agents." Journal of Medicinal Chemistry 54, no. 5 (March 10, 2011): 1276–87. http://dx.doi.org/10.1021/jm101225g.

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43

Papadopoulou, Maria V., William D. Bloomer, Howard S. Rosenzweig, Eric Chatelain, Marcel Kaiser, Shane R. Wilkinson, Caroline McKenzie, and Jean-Robert Ioset. "Novel 3-Nitro-1H-1,2,4-triazole-Based Amides and Sulfonamides as Potential Antitrypanosomal Agents." Journal of Medicinal Chemistry 55, no. 11 (May 23, 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 (June 8, 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. Molecular docking simulations revealed that four compounds (1, 9, 12 and 21) were found to similarly occupy the hydrophobic active site of trans-2-enoyl acyl carrier protein reductase of P. falciparum (PfENR) as triclosan and outcomes were closely related to their anti-malarial potencies. Results and Conclusion: The screening results against T. cruzi, T. brucei, L. donovani, L. infantum, P. falciferum and cytotoxicity assays provided a few significant to most potent compounds; two variant class of NTDs.

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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 (October 11, 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 design and a series of peptidic and non-peptidic carbohydrate-binding agents have been identified as antiparasitics showing efficacy in animal models of sleeping sickness. Here we provide an overview of the nature of surface glycans in three kinetoplastid parasites, T. cruzi, T. brucei and Leishmania. Their role in virulence and host cell invasion is highlighted with the aim of identifying specific glycan–lectin interactions and carbohydrate functions that may be the target of novel carbohydrate-binding agents with therapeutic applications.

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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 (October 19, 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 trypanocidal profile indicates that isothiochromenothiazole derivatives may be promising for designing new antitrypanosomal drugs.

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Oluwafemi, Awotunde J., Emmanuel O. Okanla, Pelayo Camps, Diego Muñoz-Torrero, Zachary B. Mackey, Peter K. Chiang, Scott Seville, and Colin W. Wright. "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 (February 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 antitrypanosomal activities with IC50 values ranging from 303-377 nM.

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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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Fernández, Mariana, Lorena Becco, Isabel Correia, Julio Benítez, Oscar E. Piro, Gustavo A. Echeverria, Andrea Medeiros, 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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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 Trypanosoma brucei brucei (T. b brucei) parasites, Plasmodium falciparum (P. falciparum) malaria parasites 3D7 strain, and human cervix adenocarcinoma cells (HeLa cells); in addition, the antimicrobial and antioxidant efficacies were determined using standard methods. Both extracts were characterized by a high amount of fatty acids (52.88 and 62.48%). The ethyl acetate extract exhibited a greater activity with minimum inhibitory concentration (MIC) values ranging from 0.025 to 0.10 mg/mL while the methanol extract ranged from 0.025 to 0.15 mg/mL. Both extracts were bactericidal to Escherichia coli ATCC 35150 (E. coli) and Pseudomonas aeruginosa ACC (P. aeruginosa). Qualitative and quantitative phytochemical screenings conducted for both extracts revealed the presence of alkaloids, glycosides, saponins, steroids, and triterpenoids, fat and oils, flavonoids, phenols, and tannins in varying amounts. Both crude extracts exhibited antitrypanosomal potentials with an IC50 of 6.6/9.7 μg/mL and antiplasmodial activities with an IC50 of 8.4/13.0 μg/mL. Conclusion from this study indicates that apart from the folkloric uses of this plant in traditional settings, the extracts possess a broad spectrum of antimicrobial, antitrypanosomal, and antimalarial activities and some pharmaceutically essential bioactive components with remarkable antioxidant capacities that may be used in the synthesis of novel drugs for the management of different varieties of ailments.

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Journal articles on the topic 'Antitrypanosomal agents'

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