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Journal articles on the topic 'Trypanocidal activity'

Author: Grafiati

Published: 4 June 2021

Last updated: 26 July 2025

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1

Enanga, Bertin, Mark R. Ariyanayagam, Mhairi L. Stewart, and Michael P. Barrett. "Activity of Megazol, a Trypanocidal Nitroimidazole, Is Associated with DNA Damage." Antimicrobial Agents and Chemotherapy 47, no. 10 (2003): 3368–70. http://dx.doi.org/10.1128/aac.47.10.3368-3370.2003.

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ABSTRACT DNA damage associated with the trypanocidal activity of megazol [2-amino-5-(1-methyl-5-nitro-2-imidazolyl)-1,3,4-thiadiazole] was shown in experiments in which DNA repair-deficient RAD51−/− Trypanosoma brucei mutants were found to be hypersensitive to the drug. Parasites resistant to megazol were selected and showed modest cross-resistance to other trypanocides, although neither drug efflux nor changes to intracellular thiols correlated with resistance.

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2

Awad, Mohamed K., Saida A. El-Enien, and Mohammed H. Rizk. "Quantitative Structure-Trypanocidal Activity Relationship Analysis of Phenothiazine Derivatives." Indian Journal of Applied Research 3, no. 9 (2011): 65–68. http://dx.doi.org/10.15373/2249555x/sept2013/20.

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3

Maciel Diogo, Gabriela, Josimara Souza Andrade, Policarpo Ademar Sales Junior, Silvane Maria Fonseca Murta, Viviane Martins Rebello Dos Santos, and Jason Guy Taylor. "Trypanocidal Activity of Flavanone Derivatives." Molecules 25, no. 2 (2020): 397. http://dx.doi.org/10.3390/molecules25020397.

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Chagas disease, also known as American trypanosomiasis, is classified as a neglected disease by the World Health Organization. For clinical treatment, only two drugs have been on the market, Benznidazole and Nifurtimox, both of which are recommended for use in the acute phase but present low cure rates in the chronic phase. Furthermore, strong side effects may result in discontinuation of this treatment. Faced with this situation, we report the synthesis and trypanocidal activity of 3-benzoyl-flavanones. Novel 3-benzoyl-flavanone derivatives were prepared in satisfactory yields in the 3-step s

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4

Boda, Caroline, Bertin Enanga, Bertrand Courtioux, J. Christian Breton, and Bernard Bouteille. "Trypanocidal Activity of Methylene Blue." Chemotherapy 52, no. 1 (2005): 16–19. http://dx.doi.org/10.1159/000090236.

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5

da Silva Filho, Ademar A., Sérgio Albuquerque, Márcio L. A. e. Silva, Marcos N. Eberlin, Daniela M. Tomazela, and Jairo K. Bastos. "Tetrahydrofuran Lignans fromNectandramegapotamicawith Trypanocidal Activity⊥." Journal of Natural Products 67, no. 1 (2004): 42–45. http://dx.doi.org/10.1021/np0302697.

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6

Ward, Christopher P., Pui Ee Wong, Richard J. Burchmore, Harry P. de Koning, and Michael P. Barrett. "Trypanocidal Furamidine Analogues: Influence of Pyridine Nitrogens on Trypanocidal Activity, Transport Kinetics, and Resistance Patterns." Antimicrobial Agents and Chemotherapy 55, no. 5 (2011): 2352–61. http://dx.doi.org/10.1128/aac.01551-10.

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ABSTRACTCurrent therapies for human African trypanosomiasis (HAT) are unsatisfactory and under threat from emerging drug resistance linked to the loss of transporters, e.g., the P2 aminopurine transporter (TbAT1). Here we compare the uptake and trypanocidal properties of furamidine (DB75), recently evaluated in clinical trials against stage 1 (haemolymphatic) HAT, and two aza analogues, DB820 and CPD0801 (DB829), which are candidate compounds for treatment of stage 2 (neurological) disease. Values of 50% inhibitory concentrations (IC50s) determinedin vitroagainst both wild-type and transporter

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7

Steverding, Dietmar, Stuart A. Rushworth, Georgina R. Hurle, et al. "Increased Trypanocidal Activity of the Salinomycin Derivative Ironomycin Is Due to ROS Production and Iron Uptake Impairment." Molecules 29, no. 23 (2024): 5597. http://dx.doi.org/10.3390/molecules29235597.

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Salinomycin and its derivatives display promising anti-proliferating activity against bloodstream forms of Trypanosoma brucei. The mechanism of trypanocidal action of these compounds is due to their ionophoretic activity inducing an influx of sodium cations followed by osmotic water uptake, leading to massive swelling of bloodstream-form trypanosomes. Generally, higher trypanocidal activities of salinomycin derivatives are associated with higher cell swelling activities. Although ironomycin (C20-propargylamine derivative of salinomycin) and salinomycin showed identical cell swelling activities

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8

Moncada-Basualto, Mauricio, Jorge Saavedra-Olavarría, Paula S. Rivero-Jerez, et al. "Assessment of the Activity of Nitroisoxazole Derivatives against Trypanosoma cruzi." Molecules 29, no. 12 (2024): 2762. http://dx.doi.org/10.3390/molecules29122762.

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The development of new compounds to treat Chagas disease is imperative due to the adverse effects of current drugs and their low efficacy in the chronic phase. This study aims to investigate nitroisoxazole derivatives that produce oxidative stress while modifying the compounds’ lipophilicity, affecting their ability to fight trypanosomes. The results indicate that these compounds are more effective against the epimastigote form of T. cruzi, with a 52 ± 4% trypanocidal effect for compound 9. However, they are less effective against the trypomastigote form, with a 15 ± 3% trypanocidal effect. Ad

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9

Ede, Samuel Otokpa, John Chinyere Aguiyi, Simeon Omale, and Rebecca Folashade Ede. "Anti-trypanosomal, antioxidant and antimicrobial activities of the fruiting bodies of Ganoderma lucidum (W. Curt.: Fr) (Ganodermataceae) aqueous extract." Journal of Pharmacy & Bioresources 18, no. 3 (2021): 172–81. http://dx.doi.org/10.4314/jpb.v18i3.1.

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Human African Trypanosomiasis (HAT) infection is caused by sub species of Trypanosoma brucei. The clinically licensed drugs have unacceptable toxicities and variable efficacies. The prognosis is influenced by the level of circulating free radicals and opportunistic infections. Many plants have been screened for activity in different models of HAT but the same is not true of mushrooms. This study screened the aqueous extract of the fruiting bodies of Ganoderma lucidum for trypanocidal, antioxidant and antimicrobial activities. Fruiting bodies of the mushroom were extracted sequentially with n –

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10

Steverding, Dietmar, Lázaro Gomes do Nascimento, Yunierkis Perez-Castillo, and Damião Pergentino de Sousa. "Gallic Acid Alkyl Esters: Trypanocidal and Leishmanicidal Activity, and Target Identification via Modeling Studies." Molecules 27, no. 18 (2022): 5876. http://dx.doi.org/10.3390/molecules27185876.

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Eight gallic acid alkyl esters (1–8) were synthesized via Fischer esterification and evaluated for their trypanocidal and leishmanicidal activity using bloodstream forms of Trypanosoma brucei and promastigotes of Leishmania major. The general cytotoxicity of the esters was evaluated with human HL-60 cells. The compounds displayed moderate to good trypanocidal but zero to low leishmanicidal activity. Gallic acid esters with alkyl chains of three or four carbon atoms in linear arrangement (propyl (4), butyl (5), and isopentyl (6)) were found to be the most trypanocidal compounds with 50% growth

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11

Liaõ, Luciano M., Gilmar A. Silva, Marcos R. Monteiro, and Sérgio Albuquerque. "Trypanocidal Activity of Quinonemethide Triterpenoids from Cheiloclinium cognatum (Hippocrateaceae)." Zeitschrift für Naturforschung C 63, no. 3-4 (2008): 207–10. http://dx.doi.org/10.1515/znc-2008-3-408.

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We report the trypanocidal activity of quinonemethide triterpenoids isolated from root extracts of Cheiloclinium cognatum, a plant of the Hippocrateaceae family, collected in the Cerrado Reserve at Universidade Federal de Goiás, Brazil. The trypanocidal activity assays showed an effect on the blood trypomastigote forms of the Y strain of Trypanosoma cruzi where tingenone and tingenol demonstrated activity on the parasite. Their structures were elucidated on the basis of spectral data, particularly COSY, HMQC and HMBC experiments, and chemical transformations

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12

Wang, Qin, Noel Murphy, and Samuel J. Black. "Infection-Associated Decline of Cape Buffalo Blood Catalase Augments Serum Trypanocidal Activity." Infection and Immunity 67, no. 6 (1999): 2797–803. http://dx.doi.org/10.1128/iai.67.6.2797-2803.1999.

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ABSTRACT Clearance of trypanosomes from the blood of infected Cape buffalo was associated with the development of two responses: (i) complement-dependent and clone-specific lytic activity and (ii) complement-independent trypanocidal activity that was not restricted by trypanosome clone or species. This latter activity was mediated by H2O2 and required the presence of xanthine oxidase in serum but not the addition of purine substrates. Expression of the xanthine oxidase-dependent trypanocidal activity in Cape buffalo serum was coincident with, and required, a decline in its H2O2catabolic activi

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13

Jones, Amy, Tanja Grkovic, Melissa Sykes, and Vicky Avery. "Trypanocidal Activity of Marine Natural Products." Marine Drugs 11, no. 10 (2013): 4058–82. http://dx.doi.org/10.3390/md11104058.

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14

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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15

Meza-Menchaca, Thuluz, Angel Ramos-Ligonio, Aracely López-Monteon, et al. "Insights into Ergosterol Peroxide’s Trypanocidal Activity." Biomolecules 9, no. 9 (2019): 484. http://dx.doi.org/10.3390/biom9090484.

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Trypanosoma cruzi, which causes Chagas disease, is a significant health threat in many countries and affects millions of people. Given the magnitude of this disease, a broader understanding of trypanocidal mechanisms is needed to prevent and treat infection. Natural endoperoxides, such as ergosterol peroxide, have been shown to be toxic to parasites without causing harm to human cells or tissues. Although prior studies have demonstrated the trypanocidal activity of ergosterol peroxide, the cellular and molecular mechanisms remain unknown. The results of this study indicate that a free-radical

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16

Stewart, Mhairi L., Gorka Jimenez Bueno, Alessandro Baliani, et al. "Trypanocidal Activity of Melamine-Based Nitroheterocycles." Antimicrobial Agents and Chemotherapy 48, no. 5 (2004): 1733–38. http://dx.doi.org/10.1128/aac.48.5.1733-1738.2004.

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ABSTRACT A series of nitroheterocyclic compounds were designed with linkages to melamine or benzamidine groups that are known substrates of the P2 aminopurine and other transporters in African trypanosomes of the brucei group. Several compounds showed in vitro trypanotoxicity with 50% inhibitory concentrations in the submicromolar range. Although most compounds interacted with the P2 transporter, as judged by their ability to inhibit adenosine transport via this carrier, uptake through this route was not necessary for activity since TbAT1-null mutant parasites, deficient in this transporter, r

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17

Ogbunugafor, Henrietta, Okochi Veronica A, Okpuzor Joy I, Titilayo Adedayo, and Stephen Esue. "Mitragyna ciliata and its trypanocidal activity." African Journal of Biotechnology 6, no. 20 (2007): 2310–13. http://dx.doi.org/10.5897/ajb2007.000-2361.

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18

Pardo Andreu, Gilberto L., Natalia M. Inada, Rolando F. Pellón, et al. "New acridinone derivative with trypanocidal activity." International Journal of Antimicrobial Agents 31, no. 5 (2008): 502–4. http://dx.doi.org/10.1016/j.ijantimicag.2008.01.015.

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19

Filho, Carlos S. M. B., Ramon R. P. P. B. de Menezes, Emanuel P. Magalhães, Yunierkis P. Castillo, Alice M. C. Martins, and Damião P. de Sousa. "Piplartine-Inspired 3,4,5-Trimethoxycinnamates: Trypanocidal, Mechanism of Action, and In Silico Evaluation." Molecules 28, no. 11 (2023): 4512. http://dx.doi.org/10.3390/molecules28114512.

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Chagas disease (CD) is one of the main neglected tropical diseases that promote relevant socioeconomic impacts in several countries. The therapeutic options for the treatment of CD are limited, and parasite resistance has been reported. Piplartine is a phenylpropanoid imide that has diverse biological activities, including trypanocidal action. Thus, the objective of the present work was to prepare a collection of thirteen esters analogous to piplartine (1–13) and evaluate their trypanocidal activity against Trypanosoma cruzi. Of the tested analogues, compound 11 ((E)-furan-2-ylmethyl 3-(3,4,5-

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20

Alcântara, Antônio Flávio de Carvalho, Damaris Silveira, Egler Chiari, Alaide Braga De Oliveira, João Edmundo Guimarães, and Delio Soares Raslan. "Comparative analysis of the trypanocidal activity and chemical properties of E-lychnophoric acid and its derivatives using theoretical calculations." Ecletica Quimica 30, no. 3 (2005): 37–45. http://dx.doi.org/10.26850/1678-4618eqj.v30.3.2005.p37-45.

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E-Lychnophoric acid 1, its derivative ester 2 and alcohol 3 killed 100% of trypomastigoteblood forms of Trypanosoma cruzi at the concentrations of 13.86, 5.68, and 6.48 μg/mL, respectively.Conformational distribution calculations (AM1) of 1, 2 and 3 gave minimum energies for the conformersa, b, c, and d, which differ from each other only in the cyclononene ring geometry. Calculations (DFT/BLYP/6-31G*) of geometry optimization and chemical properties were performed for conformers of 1, 2,and 3. The theoretical results were numerically compared to the trypanocidal activity. Calculated valuesof a

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21

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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22

Munsimbwe, Linous, Anna Seetsi, Boniface Namangala, David D. N’Da, Noboru Inoue, and Keisuke Suganuma. "In Vitro and In Vivo Trypanocidal Efficacy of Synthesized Nitrofurantoin Analogs." Molecules 26, no. 11 (2021): 3372. http://dx.doi.org/10.3390/molecules26113372.

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African trypanosomes cause diseases in humans and livestock. Human African trypanosomiasis is caused by Trypanosoma brucei rhodesiense and T. b. gambiense. Animal trypanosomoses have major effects on livestock production and the economy in developing countries, with disease management depending mainly on chemotherapy. Moreover, only few drugs are available and these have adverse effects on patients, are costly, show poor accessibility, and parasites develop drug resistance to them. Therefore, novel trypanocidal drugs are urgently needed. Here, the effects of synthesized nitrofurantoin analogs

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23

Nnadi, Charles, Godwin Ebiloma, Jennifer Black, et al. "Potent Antitrypanosomal Activities of 3-Aminosteroids against African Trypanosomes: Investigation of Cellular Effects and of Cross-Resistance with Existing Drugs." Molecules 24, no. 2 (2019): 268. http://dx.doi.org/10.3390/molecules24020268.

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Treatment of animal African trypanosomiasis (AAT) requires urgent need for safe, potent and affordable drugs and this has necessitated this study. We investigated the trypanocidal activities and mode of action of selected 3-aminosteroids against Trypanosoma brucei brucei. The in vitro activity of selected compounds of this series against T. congolense (Savannah-type, IL3000), T. b. brucei (bloodstream trypomastigote, Lister strain 427 wild-type (427WT)) and various multi-drug resistant cell lines was assessed using a resazurin-based cell viability assay. Studies on mode of antitrypanosomal act

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24

Pereira, S., D. A. Dias, S. V. Sampaio, S. C. França, M. P. A. Toldo, and S. Albuquerque. "TRYPANOCIDAL ACTIVITY FROM TABERNAEMONTANA CATHARINENSIS A. DC." Acta Horticulturae, no. 501 (February 1999): 165–70. http://dx.doi.org/10.17660/actahortic.1999.501.24.

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25

Ventura Pinto, Antônio, and Solange Lisboa de Castro. "The Trypanocidal Activity of Naphthoquinones: A Review." Molecules 14, no. 11 (2009): 4570–90. http://dx.doi.org/10.3390/molecules14114570.

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26

Donkor, Isaac O., Tien L. Huang, Bin Tao, et al. "Trypanocidal Activity of Conformationally Restricted Pentamidine Congeners." Journal of Medicinal Chemistry 46, no. 6 (2003): 1041–48. http://dx.doi.org/10.1021/jm020375q.

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27

Prytzyk, Eliane, Andreia P. Dantas, Kelly Salomão, et al. "Flavonoids and trypanocidal activity of Bulgarian propolis." Journal of Ethnopharmacology 88, no. 2-3 (2003): 189–93. http://dx.doi.org/10.1016/s0378-8741(03)00210-1.

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28

Yoshihara, Eisaku, Hiroshi Tachibana, and Taiji Nakae. "Trypanocidal activity of the stearylamine-bearing liposome." Life Sciences 40, no. 22 (1987): 2153–59. http://dx.doi.org/10.1016/0024-3205(87)90005-1.

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29

Dreyfuss, G., DP Allais, H. Guinaudeau, and J. Bruneton. "Trypanocidal activity of isoquinoline alkaloids in mice." Journal of Ethnopharmacology 23, no. 2-3 (1988): 350. http://dx.doi.org/10.1016/0378-8741(88)90062-1.

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30

Steverding, Dietmar, Lazare S. Sidjui, Éden Ramalho Ferreira, et al. "Trypanocidal and leishmanicidal activity of six limonoids." Journal of Natural Medicines 74, no. 3 (2020): 606–11. http://dx.doi.org/10.1007/s11418-020-01408-7.

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Abstract Six limonoids [kotschyienone A and B (1, 2), 7-deacetylgedunin (3), 7-deacetyl-7-oxogedunin (4), andirobin (5) and methyl angolensate (6)] were investigated for their trypanocidal and leishmanicidal activities using bloodstream forms of Trypanosoma brucei and promastigotes of Leishmania major. Whereas all compounds showed anti-trypanosomal activity, only compounds 1–4 displayed anti-leishmanial activity. The 50% growth inhibition (GI50) values for the trypanocidal and leishmanicidal activity of the compounds ranged between 2.5 and 14.9 μM. Kotschyienone A (1) was found to be the most

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31

Kiuchi, Fumiyuki, Yoshiaki Itano, Nahoko Uchiyama, et al. "Monoterpene Hydroperoxides with Trypanocidal Activity fromChenopodium ambrosioides." Journal of Natural Products 65, no. 4 (2002): 509–12. http://dx.doi.org/10.1021/np010445g.

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Alcântara, A. F. C., D. Silveira, E. Chiari, A. B. Oliveira, J. E. Guimarães, and D. S. Raslan. "Comparative analysis of the trypanocidal activity and chemical properties of E-lychnophoric acid and its derivatives using theoretical calculations." Eclética Química 30, no. 3 (2005): 37–45. http://dx.doi.org/10.1590/s0100-46702005000300005.

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E-Lychnophoric acid 1, its derivative ester 2 and alcohol 3 killed 100% of trypomastigote blood forms of Trypanosoma cruzi at the concentrations of 13.86, 5.68, and 6.48 µg/mL, respectively. Conformational distribution calculations (AM1) of 1, 2 and 3 gave minimum energies for the conformers a, b, c, and d, which differ from each other only in the cyclononene ring geometry. Calculations (DFT/BLYP/6-31G*) of geometry optimization and chemical properties were performed for conformers of 1, 2, and 3. The theoretical results were numerically compared to the trypanocidal activity. Calculated values

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33

Kaiser, Marcel, Michael A. Bray, Monica Cal, Bernadette Bourdin Trunz, Els Torreele, and Reto Brun. "Antitrypanosomal Activity of Fexinidazole, a New Oral Nitroimidazole Drug Candidate for Treatment of Sleeping Sickness." Antimicrobial Agents and Chemotherapy 55, no. 12 (2011): 5602–8. http://dx.doi.org/10.1128/aac.00246-11.

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ABSTRACTFexinidazole is a 5-nitroimidazole drug currently in clinical development for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species of the protozoan parasiteTrypanosoma brucei. The compound and its two principal metabolites, sulfoxide and sulfone, have been assessed for their ability to kill a range ofT. bruceiparasite strainsin vitroand to cure both acute and chronic HAT disease models in the mouse. The parent molecule and both metabolites have shown trypanocidal activityin vitroin the 0.7-to-3.3 μM (0.2-to-0.9 μg/ml) range ag

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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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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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Daliry, A., M. Q. Pires, C. F. Silva, et al. "The Trypanocidal Activity of Amidine Compounds Does Not Correlate with Their Binding Affinity to Trypanosoma cruzi Kinetoplast DNA." Antimicrobial Agents and Chemotherapy 55, no. 10 (2011): 4765–73. http://dx.doi.org/10.1128/aac.00229-11.

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ABSTRACTDue to limited efficacy and considerable toxicity, the therapy for Chagas' disease is far from being ideal, and thus new compounds are desirable. Diamidines and related compounds such as arylimidamides have promising trypanocidal activity againstTrypanosoma cruzi. To better understand the mechanism of action of these heterocyclic cations, we investigated the kinetoplast DNA (kDNA) binding properties and trypanocidal efficacy againstT. cruziof 13 compounds. Four diamidines (DB75, DB569, DB1345, and DB829), eight arylimidamides (DB766, DB749, DB889, DB709, DB613, DB1831, DB1852, and DB20

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37

Silva, Rayanne H. N., Emanuel P. Magalhães, Rebeca C. Gomes, Yunierkis Perez-Castillo, Alice M. C. Martins, and Damião P. de Sousa. "Piplartine Synthetic Analogs: In Silico Analysis and Antiparasitic Study against Trypanosoma cruzi." Applied Sciences 13, no. 20 (2023): 11585. http://dx.doi.org/10.3390/app132011585.

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Neglected tropical diseases (NTDs) cause thousands of deaths each year. Among these diseases, we find Chagas disease, whose etiologic agent is Trypanosoma cruzi. Piplartine is an alkamide present in various species of the genus Piper that possess trypanocidal activity. In this study, the antiparasitic potential of a collection of 23 synthetic analogs of piplartine against Trypanosoma cruzi was evaluated in vitro. The compounds were prepared via amidation and esterification reactions using 3,4,5-trimethoxybenzoic acid as starting material. The products were structurally characterized using 1H a

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38

Gopi, Elumalai, Tarun Kumar, Rubem F. S. Menna-Barreto, Wagner O. Valença, Eufrânio N. da Silva Júnior та Irishi N. N. Namboothiri. "Imidazoles from nitroallylic acetates and α-bromonitroalkenes with amidines: synthesis and trypanocidal activity studies". Organic & Biomolecular Chemistry 13, № 38 (2015): 9862–71. http://dx.doi.org/10.1039/c5ob01444a.

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González, Luis A., Sara Robledo, Yulieth Upegui, Gustavo Escobar, and Wiston Quiñones. "Synthesis and Evaluation of Trypanocidal Activity of Chromane-Type Compounds and Acetophenones." Molecules 26, no. 23 (2021): 7067. http://dx.doi.org/10.3390/molecules26237067.

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American trypanosomiasis (Chagas disease) caused by the Trypanosoma cruzi parasite, is a severe health problem in different regions of Latin America and is currently reported to be spreading to Europe, North America, Japan, and Australia, due to the migration of populations from South and Central America. At present, there is no vaccine available and chemotherapeutic options are reduced to nifurtimox and benznidazole. Therefore, the discovery of new molecules is urgently needed to initiate the drug development process. Some acetophenones and chalcones, as well as chromane-type substances, such

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Costa, Emmanoel Vilaça, Lívia Macedo Dutra, Paulo Cesar de Lima Nogueira, et al. "Essential Oil from the Leaves of Annona vepretorum: Chemical Composition and Bioactivity." Natural Product Communications 7, no. 2 (2012): 1934578X1200700. http://dx.doi.org/10.1177/1934578x1200700240.

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The essential oil from the leaves of Annona vepretorun was obtained by hydrodistillation using a Clevenger-type apparatus and analyzed by GC-MS and GC-FID. Eighteen compounds representing 98.1% of the crude essential oil were identified. The major compounds identified were bicyclogermacrene (43.7%), spathulenol (11.4%), α-felandrene (10.0%), α-pinene (7.1%), (E)-β-ocimene (6.8%), germacrene D (5.8%), and p-cymene (4.2%). The trypanocidal activity against Trypanosoma cruzi epimastigote forms, as well as, the antimicrobial and antioxidant proprieties was investigated. The essential oil showed a

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Foscolos, Angeliki-Sofia, Ioannis Papanastasiou, George B. Foscolos, et al. "New hydrazones of 5-nitro-2-furaldehyde with adamantanealkanohydrazides: synthesis and in vitro trypanocidal activity." MedChemComm 7, no. 6 (2016): 1229–36. http://dx.doi.org/10.1039/c6md00035e.

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Herráez, Rocío, Roberto Quesada, Norma Dahdah, Miguel Viñas, and Teresa Vinuesa. "Tambjamines and Prodiginines: Biocidal Activity against Trypanosoma cruzi." Pharmaceutics 13, no. 5 (2021): 705. http://dx.doi.org/10.3390/pharmaceutics13050705.

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The aim of this work was to explore new therapeutic options against Chagas disease by the in vitro analysis of the biocidal activities of several tambjamine and prodiginine derivatives, against the Trypanosoma cruzi CLB strain (DTU TcVI). The compounds were initially screened against epimastigotes. The five more active compounds were assayed in intracellular forms. The tambjamine MM3 and both synthetic and natural prodigiosins displayed the highest trypanocidal profiles, with IC50 values of 4.52, 0.46, and 0.54 µM for epimastigotes and 1.9, 0.57, and 0.1 µM for trypomastigotes/amastigotes, res

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LIMA, LUCIANA A. R. S., TÂNIA M. A. ALVES, CARLOS L. ZANI, et al. "In vitro cytotoxic, antifungal, trypanocidal and leishmanicidal activities of acetogenins isolated from Annona cornifolia A. St. -Hil. (Annonaceae)." Anais da Academia Brasileira de Ciências 86, no. 2 (2014): 829–39. http://dx.doi.org/10.1590/0001-3765201420130048.

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Annona cornifolia A. St. -Hil. is a small annual perennial tree found in the Brazilian savannah; their green fruit is popularly used in the treatment of ulcers. The acetogenins isolated from the seeds of Annona cornifolia previously showed to possess antioxidant activity. In continuation of our investigations on the biological activities of acetogenins, four binary mixtures and ten pure adjacent bis-tetrahydrofuran annonaceous acetogenins were evaluated: the cytotoxic (against three human tumor cell lines), antifungal (against Paracoccidioides brasiliensis), trypanocidal (against Trypanosoma c

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Hall, Belinda S., Emma Louise Meredith, and Shane R. Wilkinson. "Targeting the Substrate Preference of a Type I Nitroreductase To Develop Antitrypanosomal Quinone-Based Prodrugs." Antimicrobial Agents and Chemotherapy 56, no. 11 (2012): 5821–30. http://dx.doi.org/10.1128/aac.01227-12.

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ABSTRACTNitroheterocyclic prodrugs are used to treat infections caused byTrypanosoma cruziandTrypanosoma brucei. A key component in selectivity involves a specific activation step mediated by a protein homologous with type I nitroreductases, enzymes found predominantly in prokaryotes. Using data from determinations based on flavin cofactor, oxygen-insensitive activity, substrate range, and inhibition profiles, we demonstrate that NTRs fromT. cruziandT. bruceidisplay many characteristics of their bacterial counterparts. Intriguingly, both enzymes preferentially use NADH and quinones as the elec

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Dantas, Elen, Fabia de Souza, William Nogueira, et al. "Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone." Molecules 22, no. 10 (2017): 1631. http://dx.doi.org/10.3390/molecules22101631.

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Ambrozin, Alessandra Regina Pepe, Paulo Cezar Vieira, João Batista Fernandes, Maria Fátima das Graças Fernandes da Silva, and Sérgio de Albuquerque. "Trypanocidal activity of Meliaceae and Rutaceae plant extracts." Memórias do Instituto Oswaldo Cruz 99, no. 2 (2004): 227–31. http://dx.doi.org/10.1590/s0074-02762004000200020.

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Mesquita, Mariana Laundry de, Julie Desrivot, Bories, et al. "Antileishmanial and trypanocidal activity of Brazilian Cerrado plants." Memórias do Instituto Oswaldo Cruz 100, no. 7 (2005): 783–87. http://dx.doi.org/10.1590/s0074-02762005000700019.

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Legarda-Ceballos, Ana, Esther del Olmo, Julio López-Abán, et al. "Trypanocidal Activity of Long Chain Diamines and Aminoalcohols." Molecules 20, no. 6 (2015): 11554–68. http://dx.doi.org/10.3390/molecules200611554.

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Steverding, Dietmar, Xia Wang, Barbara Potts та Michael Palladino. "Trypanocidal Activity ofβ-Lactone-γ-Lactam Proteasome Inhibitors". Planta Medica 78, № 02 (2011): 131–34. http://dx.doi.org/10.1055/s-0031-1280315.

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Shuaibu, M. N., D. A. Ameh, J. J. Bonire, A. O. Adaudi, S. Ibrahim, and A. J. Nok. "Trypanocidal activity of organotin chlorides onTrypanosomabrucei-infected mice." Parasite 7, no. 1 (2000): 43–45. http://dx.doi.org/10.1051/parasite/2000071043.

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