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Journal articles on the topic 'Antiprotozoal agents'

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1

Graebin, C., F. Uchoa, L. Bernardes, V. Campo, I. Carvalho, and V. Eifler-Lima. "Antiprotozoal Agents: An Overview." Anti-Infective Agents in Medicinal Chemistry 8, no. 4 (October 1, 2009): 345–66. http://dx.doi.org/10.2174/187152109789760199.

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Chibale, Kelly. "Towards broadspectrum antiprotozoal agents." Arkivoc 2002, no. 9 (January 17, 2003): 93–98. http://dx.doi.org/10.3998/ark.5550190.0003.910.

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3

Phillipson, J., and Colin Wright. "Antiprotozoal Agents from Plant Sources." Planta Medica 57, S 1 (October 1991): S53—S59. http://dx.doi.org/10.1055/s-2006-960230.

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4

Khaw, M., and C. B. Panosian. "Human antiprotozoal therapy: past, present, and future." Clinical Microbiology Reviews 8, no. 3 (July 1995): 427–39. http://dx.doi.org/10.1128/cmr.8.3.427.

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Human protozoal infections are ubiquitous and occur worldwide. In many cases, antiprotozoal agents currently in use predate the modern antibiotic era. Despite the relative lag in development of new antiprotozoal agents, the 1990s have witnessed an increasing level of interest in these infections, inspired by international travel and immigration, a growing awareness of antiprotozoal drug resistance, and the significance of acute and recrudescent protozoal infections in immunosuppressed hosts. This review summarizes for nonclinician readers the past, present, and future therapies for common human protozoal infections, as well as pharmacologic mechanisms of action and resistance and common toxicities associated with these agents.
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5

McClure, C. D., and Linda L. Nolan. "HERB EXTRACTS AS POTENTIAL ANTIPROTOZOAL AGENTS." Acta Horticulturae, no. 426 (August 1996): 91–104. http://dx.doi.org/10.17660/actahortic.1996.426.10.

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6

Ismail, Mohamed A., Reto Brun, Tanja Wenzler, Farial A. Tanious, W. David Wilson, and David W. Boykin. "Dicationic biphenyl benzimidazole derivatives as antiprotozoal agents." Bioorganic & Medicinal Chemistry 12, no. 20 (October 2004): 5405–13. http://dx.doi.org/10.1016/j.bmc.2004.07.056.

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Bassanini, Ivan, Silvia Parapini, Nicoletta Basilico, and Anna Sparatore. "Novel Hydrophilic Riminophenazines as Potent Antiprotozoal Agents." ChemMedChem 14, no. 22 (November 5, 2019): 1940–49. http://dx.doi.org/10.1002/cmdc.201900522.

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8

Mendonça-Junior, Francisco Jaime Bezerra. "Special Issue “Drug Discovery of Antiprotozoal Agents”." Pharmaceuticals 17, no. 2 (January 30, 2024): 176. http://dx.doi.org/10.3390/ph17020176.

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Protozoal diseases, such as leishmaniasis, malaria, African sleeping sickness, Chagas disease, amoebiasis, giardiasis, cryptococcosis, and toxoplasmosis (among others), affect and/or have the potential to infect more than one billion people worldwide [...]
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9

Lee, Kim, Hayat, and Shin. "Recent Advances in the Discovery of Novel Antiprotozoal Agents." Molecules 24, no. 21 (October 28, 2019): 3886. http://dx.doi.org/10.3390/molecules24213886.

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Parasitic diseases have serious health, social, and economic impacts, especially in the tropical regions of the world. Diseases caused by protozoan parasites are responsible for considerable mortality and morbidity, affecting more than 500 million people worldwide. Globally, the burden of protozoan diseases is increasing and is been exacerbated because of a lack of effective medication due to the drug resistance and toxicity of current antiprotozoal agents. These limitations have prompted many researchers to search for new drugs against protozoan parasites. In this review, we have compiled the latest information (2012–2017) on the structures and pharmacological activities of newly developed organic compounds against five major protozoan diseases, giardiasis, leishmaniasis, malaria, trichomoniasis, and trypanosomiasis, with the aim of showing recent advances in the discovery of new antiprotozoal drugs.
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10

Upadhayaya, Ram Shankar, Shailesh S. Dixit, Andras Földesi, and Jyoti Chattopadhyaya. "New antiprotozoal agents: Their synthesis and biological evaluations." Bioorganic & Medicinal Chemistry Letters 23, no. 9 (May 2013): 2750–58. http://dx.doi.org/10.1016/j.bmcl.2013.02.054.

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11

Inam, Afreen, Robyn L. Van Zyl, Natasha J. van Vuuren, Chien-Teng Chen, Fernando Avecilla, Subhash M. Agarwal, and Amir Azam. "Chloroquinoline–acetamide hybrids: a promising series of potential antiprotozoal agents." RSC Advances 5, no. 60 (2015): 48368–81. http://dx.doi.org/10.1039/c5ra05472a.

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In an endeavour to develop efficacious antiprotozoal agents chloroquinoline–acetamide hybrids were synthesized and screened in vitro against E. histolytica and P. falciparum and molecular docking studies were performed against PfDHFR.
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12

Fidalgo, Lianet Monzote, Idalia Sariego Ramos, Marley García Parra, Osmany Cuesta-Rubio, Ingrid Márquez Hernández, Mercedes Campo Fernández, Anna Lisa Piccinelli, and Luca Rastrelli. "Activity of Cuban Propolis Extracts on Leishmania Amazonensis and Trichomonas vaginalis." Natural Product Communications 6, no. 7 (July 2011): 1934578X1100600. http://dx.doi.org/10.1177/1934578x1100600712.

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In this paper we analyzed the antiprotozoal effects of eighteen Cuban propolis extracts (brown, red and yellow type) collected in different geographic areas, using Leishmania amazonensis (as a model of intracellular protozoa) and Trichomonas vaginalis (as a model of extracellular protozoa). All evaluated propolis extracts caused inhibitory effect on intracellular amastigotes of L. amazonensis. However, cytotoxicity on peritoneal macrophages from BALB/c mice was observed. Only five samples decreased the viability of T. vaginalis trophozoites at concentrations lower than 10 μg/mL. No correlation between the type of propolis and antiprotozoal activity was found. Cuban propolis extracts demonstrated activity against both intracellular and extracellular protozoa model, as well as the potentialities of propolis as a natural source to obtain new antiprotozoal agents.
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Estrella-Parra, Edgar Antonio, Rodrigo Arreola, Maria Elizbeth Álvarez-Sánchez, Julio César Torres-Romero, Oscar Rojas-Espinosa, José Alberto De la Cruz-Santiago, Máximo Berto Martinez-Benitez, et al. "Natural marine products as antiprotozoal agents against amitochondrial parasites." International Journal for Parasitology: Drugs and Drug Resistance 19 (August 2022): 40–46. http://dx.doi.org/10.1016/j.ijpddr.2022.05.003.

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14

Meinke, Peter, and Paul Liberator. "Histone Deacetylase: A Target for Antiproliferative and Antiprotozoal Agents." Current Medicinal Chemistry 8, no. 2 (February 1, 2001): 211–35. http://dx.doi.org/10.2174/0929867013373787.

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15

Fernandes, Vitória de Souza, Rafael Rosa, Lara A. Zimmermann, Kamilla R. Rogério, Arthur E. Kümmerle, Lilian S. C. Bernardes, and Cedric S. Graebin. "Antiprotozoal agents: How have they changed over a decade?" Archiv der Pharmazie 355, no. 2 (October 18, 2021): 2100338. http://dx.doi.org/10.1002/ardp.202100338.

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16

Bakunova, Svetlana M., Stanislav A. Bakunov, Donald A. Patrick, E. V. K. Suresh Kumar, Kwasi A. Ohemeng, Arlene S. Bridges, Tanja Wenzler, et al. "Structure−Activity Study of Pentamidine Analogues as Antiprotozoal Agents." Journal of Medicinal Chemistry 52, no. 7 (April 9, 2009): 2016–35. http://dx.doi.org/10.1021/jm801547t.

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17

Ismail, Mohamed A., Serry A. El Bialy, Reto Brun, Tanja Wenzler, Rupesh Nanjunda, W. David Wilson, and David W. Boykin. "Dicationic phenyl-2,2′-bichalcophenes and analogues as antiprotozoal agents." Bioorganic & Medicinal Chemistry 19, no. 2 (January 2011): 978–84. http://dx.doi.org/10.1016/j.bmc.2010.11.047.

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18

Chackal-Catoen, Sarah, Yi Miao, W. David Wilson, Tanja Wenzler, Reto Brun, and David W. Boykin. "Dicationic DNA-targeted antiprotozoal agents: Naphthalene replacement of benzimidazole." Bioorganic & Medicinal Chemistry 14, no. 22 (November 2006): 7434–45. http://dx.doi.org/10.1016/j.bmc.2006.07.024.

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19

CREEK, DARREN J., and MICHAEL P. BARRETT. "Determination of antiprotozoal drug mechanisms by metabolomics approaches." Parasitology 141, no. 1 (June 5, 2013): 83–92. http://dx.doi.org/10.1017/s0031182013000814.

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SUMMARYThe discovery, development and optimal utilization of pharmaceuticals can be greatly enhanced by knowledge of their modes of action. However, many drugs currently on the market act by unknown mechanisms. Untargeted metabolomics offers the potential to discover modes of action for drugs that perturb cellular metabolism. Development of high resolution LC-MS methods and improved data analysis software now allows rapid detection of drug-induced changes to cellular metabolism in an untargeted manner. Several studies have demonstrated the ability of untargeted metabolomics to provide unbiased target discovery for antimicrobial drugs, in particular for antiprotozoal agents. Furthermore, the utilization of targeted metabolomics techniques has enabled validation of existing hypotheses regarding antiprotozoal drug mechanisms. Metabolomics approaches are likely to assist with optimization of new drug candidates by identification of drug targets, and by allowing detailed characterization of modes of action and resistance of existing and novel antiprotozoal drugs.
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20

Riscoe, M. K., A. J. Ferro, and J. H. Fitchen. "Analogs of 5-methylthioribose, a novel class of antiprotozoal agents." Antimicrobial Agents and Chemotherapy 32, no. 12 (December 1, 1988): 1904–6. http://dx.doi.org/10.1128/aac.32.12.1904.

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21

Biftu, Tesfaye, Dennis Feng, Michael Fisher, Gui-Bai Liang, Xiaoxia Qian, Andrew Scribner, Richard Dennis, et al. "Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents." Bioorganic & Medicinal Chemistry Letters 16, no. 9 (May 2006): 2479–83. http://dx.doi.org/10.1016/j.bmcl.2006.01.092.

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22

Moreno-Herrera, Antonio. "Recent Advances in the Development of Broad-Spectrum Antiprotozoal Agents." Current Medicinal Chemistry 28, no. 3 (2021): 583–606. http://dx.doi.org/10.2174/1875533xmta0eotgs5.

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23

Kalt, Marc-Manuel, Wolfgang Schuehly, Robert Saf, Sandra Ochensberger, Julia Solnier, Franz Bucar, Marcel Kaiser, and Armin Presser. "Palladium-catalysed synthesis of arylnaphthoquinones as antiprotozoal and antimycobacterial agents." European Journal of Medicinal Chemistry 207 (December 2020): 112837. http://dx.doi.org/10.1016/j.ejmech.2020.112837.

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24

Knight, B., R. Abraham, S. W. Page, and S. Abraham. "48: DRUG SCREENING OF NOVEL ANTIPROTOZOAL AGENTS AGAINST GIARDIA DUODENALIS." Journal of Global Antimicrobial Resistance 31 (December 2022): S29. http://dx.doi.org/10.1016/s2213-7165(22)00327-7.

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25

Basly, J. P., I. Longy, and M. Bernard. "Influence of radiation treatment on two antibacterial agents and four antiprotozoal agents: ESR dosimetry." International Journal of Pharmaceutics 154, no. 1 (August 1997): 109–13. http://dx.doi.org/10.1016/s0378-5173(97)00119-1.

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26

Iwiński, Hubert, Jacek Łyczko, Henryk Różański, and Antoni Szumny. "Novel Formula of Antiprotozoal Mixtures." Antibiotics 11, no. 7 (July 7, 2022): 913. http://dx.doi.org/10.3390/antibiotics11070913.

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Antimicrobial resistance (AMR) is becoming more common in both bacteria and pathogenic protozoa. Therefore, new solutions are being sought as alternatives to currently used agents. There are many new ideas and solutions, especially compounds of natural origin, including essential oils. In the present study, the antiprotozoal activity of a mixture of essential oils (eucalyptus, lavender, cedar and tea tree), organic acids (acetic acid, propionic acid and lactic acid) and metal ions (Cu, Zn, Mn) were tested. As a model, protozoans were selected: Euglena gracilis, Gregarina blattarum, Amoeba proteus, Paramecium caudatum, Pentatrichomonas hominis. The tested concentrations of mixtures were in the range of 0.001–1.5%. The analyses show unexpected, very strong protozoicidal activity of combinations, presenting the synergy of compounds via determination of LD50 and LD100 values. Obtained mixtures showed significantly higher activity against protozoans, compared to chloramphenicol and metronidazole. Most of the analyzed samples show high antiprotozoal activity at very low concentration, in the range of 0.001–0.009%. The most effective combinations for all analyzed protozoans were the cedar essential oil and tea tree essential oil with a mixture of acids and manganese or zinc ions. Innovative combinations of essential oils, organic acids and metal ions are characterized by very high antiprotozoal activity at low doses, which, after further investigation, can be applicable for control of protozoan pathogens.
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27

Abdelgawad, Mohamed A., Mohammad M. Al-Sanea, Mohamed A. Zaki, Enas I. A. Mohamed, Shabana I. Khan, Babu L. Tekwani, Amar G. Chittiboyina, et al. "New Benzoxazole Derivatives as Antiprotozoal Agents: In Silico Studies, Synthesis, and Biological Evaluation." Journal of Chemistry 2021 (March 3, 2021): 1–11. http://dx.doi.org/10.1155/2021/6631868.

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Background. Benzoxazole derivatives have different biological activities. In pursuit of designing novel chemical entities with antiprotozoal and antimicrobial activities, benzoxazolyl aniline was utilized as a privileged scaffold of a series of (3-benzoxazole-2-yl) phenylamine derivatives, 3-benzoxazoloyl acetamide, and butyramide derivatives. Methods. These novel analogs were synthesized in straightforward simple chemistry without any quantitative chromatographic separations in reasonable yields. The biological evaluation of all target compounds as potential antimalarial, antileishmanial, antitrypanosomal, and antimicrobial agents was performed by various well-established cell-based methods. Results. Compounds 6d and 5a showed promising biological screening data. The amidation of 3-benzoxazolyl aniline 1 with the chloroacetyl functional group resulted in a good antimalarial activity and showed moderate inhibitory activities against leishmanial and trypanosomal spp. Moreover, chloroacetyl functionalization of benzoxazolyl aniline serves as a good early goal for constructing and synthesizing new antimicrobial and antiprotozoal agents. The molecular docking study rationalizes the relative inhibitory activity of compound 5a as an antimalarial agent with the deregulation of PfPNP activity which has emerged as a major mechanism of these targets.
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Khandazhinskaya, Anastasia, Elena Matyugina, Pavel Solyev, Maggie Wilkinson, Karen Buckheit, Robert Buckheit, Larisa Chernousova, et al. "Investigation of 5’-Norcarbocyclic Nucleoside Analogues as Antiprotozoal and Antibacterial Agents." Molecules 24, no. 19 (September 21, 2019): 3433. http://dx.doi.org/10.3390/molecules24193433.

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Carbocyclic nucleosides have long played a role in antiviral, antiparasitic, and antibacterial therapies. Recent results from our laboratories from two structurally related scaffolds have shown promising activity against both Mycobacterium tuberculosis and several parasitic strains. As a result, a small structure activity relationship study was designed to further probe their activity and potential. Their synthesis and the results of the subsequent biological activity are reported herein.
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Ismail, Mohamed A., Adalgisa Batista-Parra, Yi Miao, W. David Wilson, Tanja Wenzler, Reto Brun, and David W. Boykin. "Dicationic near-linear biphenyl benzimidazole derivatives as DNA-targeted antiprotozoal agents." Bioorganic & Medicinal Chemistry 13, no. 24 (December 2005): 6718–26. http://dx.doi.org/10.1016/j.bmc.2005.07.024.

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30

Bernal, Freddy A., Marcel Kaiser, Bernhard Wünsch, and Thomas J. Schmidt. "Structure−Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents." ChemMedChem 15, no. 1 (November 12, 2019): 68–78. http://dx.doi.org/10.1002/cmdc.201900544.

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31

Lukáč, Miloš, Lívia Slobodníková, Martin Mrva, Aneta Dušeková, Mária Garajová, Martin Kello, Dominika Šebová, et al. "Caffeic Acid Phosphanium Derivatives: Potential Selective Antitumor, Antimicrobial and Antiprotozoal Agents." International Journal of Molecular Sciences 25, no. 2 (January 18, 2024): 1200. http://dx.doi.org/10.3390/ijms25021200.

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Caffeic acid (CA) is one of the most abundant natural compounds present in plants and has a broad spectrum of beneficial pharmacological activities. However, in some cases, synthetic derivation of original molecules can expand their scope. This study focuses on the synthesis of caffeic acid phosphanium derivatives with the ambition of increasing their biological activities. Four caffeic acid phosphanium salts (CAPs) were synthesized and tested for their cytotoxic, antibacterial, antifungal, and amoebicidal activity in vitro, with the aim of identifying the best area for their medicinal use. CAPs exhibited significantly stronger cytotoxic activity against tested cell lines (HeLa, HCT116, MDA-MB-231 MCF-7, A2058, PANC-1, Jurkat) in comparison to caffeic acid. Focusing on Jurkat cells (human leukemic T cell lymphoma), the IC50 value of CAPs ranged from 0.9 to 8.5 μM while IC50 of CA was >300 μM. Antimicrobial testing also confirmed significantly higher activity of CAPs against selected microbes in comparison to CA, especially for Gram-positive bacteria (MIC 13–57 μM) and the yeast Candida albicans (MIC 13–57 μM). The anti-Acanthamoeba activity was studied against two pathogenic Acanthamoeba strains. In the case of A. lugdunensis, all CAPs revealed a stronger inhibitory effect (EC50 74–3125 μM) than CA (>105 µM), while in A. quina strain, the higher inhibition was observed for three derivatives (EC50 44–291 μM). The newly synthesized quaternary phosphanium salts of caffeic acid exhibited selective antitumor action and appeared to be promising antimicrobial agents for topical application, as well as potential molecules for further research.
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Cardona-G, Wilson, Andres F. Yepes, and Angie Herrera-R. "Hybrid Molecules: Promising Compounds for the Development of New Treatments Against Leishmaniasis and Chagas Disease." Current Medicinal Chemistry 25, no. 30 (September 27, 2018): 3637–79. http://dx.doi.org/10.2174/0929867325666180309111428.

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Leishmaniasis and Chagas disease are endemic pathologies in tropical countries. These cause high morbidity and a public health problem. Current chemotherapies are based on conventional drugs with variable efficacy and toxicity related with the length of therapeutic schemes and high doses. When two pharmacological agents are combined into a single molecule, the result is the so-called hybrid molecule. In the search for new treatments against Chagas disease and leishmaniasis, several studies have shown that hybrid molecules display high antiprotozoal activity and this emerging strategy is quite promising in the field of new drug discovery and development. This review focuses on the antiprotozoal activity of different hybrids obtained from the hybridization of pharmacophores, showing that the most of the efforts have been concentrated in the molecular hybridization of quinoline, chalcone and hydrazone moieties.
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33

Lunardi, Fabiane, Michel Guzela, Andrea T. Rodrigues, Rogério Corrêa, Iriane Eger-Mangrich, Mário Steindel, Edmundo C. Grisard, Jamil Assreuy, João B. Calixto, and Adair R. S. Santos. "Trypanocidal and Leishmanicidal Properties of Substitution-Containing Chalcones." Antimicrobial Agents and Chemotherapy 47, no. 4 (April 2003): 1449–51. http://dx.doi.org/10.1128/aac.47.4.1449-1451.2003.

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ABSTRACT Ten chalcones were synthesized and tested as potential leishmanicidal and trypanocidal agents. All tested compounds caused concentration-dependent inhibition of the in vitro growth of Leishmania braziliensis and Trypanosoma cruzi with no significant toxic effect towards host macrophages. Our results show that the positions of the substituents seem to be critical for their antiprotozoal activities.
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Kajal, Anu, Suman Bala, Neha Sharma, Sunil Kamboj, and Vipin Saini. "Therapeutic Potential of Hydrazones as Anti-Inflammatory Agents." International Journal of Medicinal Chemistry 2014 (March 4, 2014): 1–11. http://dx.doi.org/10.1155/2014/761030.

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Hydrazones are a special class of organic compounds in the Schiff base family. Hydrazones constitute a versatile compound of organic class having basic structure (R1R2C=NNR3R4). The active centers of hydrazone, that is, carbon and nitrogen, are mainly responsible for the physical and chemical properties of the hydrazones and, due to the reactivity toward electrophiles and nucleophiles, hydrazones are used for the synthesis of organic compound such as heterocyclic compounds with a variety of biological activities. Hydrazones and their derivatives are known to exhibit a wide range of interesting biological activities like antioxidant, anti-inflammatory, anticonvulsant, analgesic, antimicrobial, anticancer, antiprotozoal, antioxidant, antiparasitic, antiplatelet, cardioprotective, anthelmintic, antidiabetic, antitubercular, trypanocidal, anti-HIV, and so forth. The present review summarizes the efficiency of hydrazones as potent anti-inflammatory agents.
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Reimão, Juliana Quero, Juliana Tonini Mesquita, Daiane Dias Ferreira, and Andre Gustavo Tempone. "Investigation of Calcium Channel Blockers as Antiprotozoal Agents and Their Interference in the Metabolism ofLeishmania (L.) infantum." Evidence-Based Complementary and Alternative Medicine 2016 (2016): 1–9. http://dx.doi.org/10.1155/2016/1523691.

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Leishmaniasis and Chagas disease are neglected parasitic diseases endemic in developing countries; efforts to find new therapies remain a priority. Calcium channel blockers (CCBs) are drugs in clinical use for hypertension and other heart pathologies. Based on previous reports about the antileishmanial activity of dihydropyridine-CCBs, this work aimed to investigate whether thein vitroanti-Leishmania infantumand anti-Trypanosoma cruziactivities of this therapeutic class would be shared by other non-dihydropyridine-CCBs. Except for amrinone, our results demonstrated antiprotozoal activity for fendiline, mibefradil, and lidoflazine, with IC50values in a range between 2 and 16 μM and Selectivity Index between 4 and 10. Fendiline demonstrated depolarization of mitochondrial membrane potential, with increased reactive oxygen species production in amlodipine and fendiline treatedLeishmania, but without plasma membrane disruption. Finally,in vitrocombinations of amphotericin B, miltefosine, and pentamidine againstL. infantumshowed in isobolograms an additive interaction when these drugs were combined with fendiline, resulting in overall mean sum of fractional inhibitory concentrations between 0.99 and 1.10. These data demonstrated that non-dihydropyridine-CCBs present antiprotozoal activity and could be useful candidates for futurein vivoefficacy studies against Leishmaniasis and Chagas’ disease.
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Amina, Musarat, Nawal M. Al Musayeib, Seham Alterary, Maha F. El-Tohamy, and Samira A. Alhwaiti. "Advanced polymeric metal/metal oxide bionanocomposite using seaweed Laurencia dendroidea extract for antiprotozoal, anticancer, and photocatalytic applications." PeerJ 11 (March 20, 2023): e15004. http://dx.doi.org/10.7717/peerj.15004.

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Background Biosynthesized nanoparticles are gaining popularity due to their distinctive biological applications as well as bioactive secondary metabolites from natural products that contribute in green synthesis. Methodology This study reports a facile, ecofriendly, reliable, and cost-effective synthesis of silver nanoparticles (AgNPs), copper oxide nanoparticles (CuONPs), and polymeric PVP-silver-copper oxide nanocomposite using ethanol extract of seaweed Laurencia dendroidea and were evaluated for antiprotozoal, anticancer and photocatalytic potential. The nanostructures of the AgNPs, CuONPs, and polymeric PVP-Ag-CuO nanocomposite were confirmed by different spectroscopic and microscopic procedures. Results The UV-vis spectrum displayed distinct absorption peaks at 440, 350, and 470 nm for AgNPs, CuONPs, and polymeric Ag-CuO nanocomposite, respectively. The average particles size of the formed AgNPs, CuONPs, and Ag-CuO nanocomposite was 25, 28, and 30 nm, respectively with zeta potential values −31.7 ± 0.6 mV, −17.6 ± 4.2 mV, and −22.9 ± 4.45 mV. The microscopic investigation of biosynthesized nanomaterials revealed a spherical morphological shape with average crystallite sizes of 17.56 nm (AgNPs), 18.21 nm (CuONPs), and 25.46 nm (PVP-Ag-CuO nanocomposite). The antiprotozoal potential of green synthesized nanomaterials was examined against Leishmania amazonensis and Trypanosoma cruzi parasites. The polymeric PVP-Ag-CuO nanocomposite exerted the highest antiprotozoal effect with IC50 values of 17.32 ± 1.5 and 17.48 ± 4.2 µM, in contrast to AgNPs and CuONPs. The anticancer potential of AgNPs, CuONPs, and polymeric PVP-Ag-CuO nanocomposite against HepG2 cancer cell lines revealed that all the nanomaterials were effective and the highest anticancer potential was displayed by PVP-Ag-CuO nanocomposite with IC50 values 91.34 µg mL−1 at 200 µg mL−1 concentration. Additionally, PVP-Ag-CuO nanocomposite showed strong photocatalytic effect. Conclusion Overall, this study suggested that the biogenic synthesized nanomaterials AgNPs, CuONPs, and polymeric PVP-Ag-CuO nanocomposite using ethanol extract of seaweed L. dendroidea possesses promising antiprotozoal anticancer and photocatalytic effect and could be further exploited for the development of antiprotozoal and anticancer therapeutics agents.
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37

Dimmock, J. R., D. W. Elias, M. A. Beazely, and N. M. Kandepu. "Bioactivities of Chalcones." Current Medicinal Chemistry 6, no. 12 (December 1999): 1125–49. http://dx.doi.org/10.2174/0929867306666220401182509.

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This review outlines the different bioactivities of a variety of chalcones. The cytotoxic, anticancer, chemopreventative and mutagenic properties of a number of chalcones are described followed by an account of various of these unsaturated ketones as antimicrobial agents. The antiviral, antiprotozoal and insecticidal activities of a variety of chalcones are reviewed as well as the enzyme-inhibitory properties and miscellaneous activities of some of these molecules.
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38

Alcalde, E., I. Dinarés, J. Elguero, J. Frigola, A. Osuna, and S. Castanys. "Pyridinium azolate betaines and their derivatives: a new class of antiprotozoal agents." European Journal of Medicinal Chemistry 25, no. 4 (May 1990): 309–19. http://dx.doi.org/10.1016/0223-5234(90)90114-i.

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39

Saccoliti, Francesco, Roberto Di Santo, and Roberta Costi. "Recent Advancement in the Search of Innovative Antiprotozoal Agents Targeting Trypanothione Metabolism." ChemMedChem 15, no. 24 (September 11, 2020): 2420–35. http://dx.doi.org/10.1002/cmdc.202000325.

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40

Pagotti, Mariana C., Herbert J. Dias, Ana Carolina B. B. Candido, Thaís A. S. Oliveira, Alexandre Borges, Nicoli D. Oliveira, Carla D. Lopes, et al. "Exploring Synthetic Dihydrobenzofuran and Benzofuran Neolignans as Antiprotozoal Agents against Trypanosoma cruzi." Pharmaceutics 15, no. 3 (February 24, 2023): 754. http://dx.doi.org/10.3390/pharmaceutics15030754.

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Chagas disease is a neglected tropical disease that affects more than 8 million people. Although there are therapies against this disease, the search for new drugs is important because the current treatments show limited effectiveness and high toxicity. In this work, eighteen dihydrobenzofuran-type neolignans (DBNs) and two benzofuran-type neolignans (BNs) were synthesized and evaluated against amastigote forms of two Trypanosoma cruzi strains. The in vitro cytotoxicity and hemolytic activity of the most active compounds were also evaluated and their relationships with T. cruzi tubulin DBNs were investigated by an in silico approach. Four DBNs demonstrated activity against the T. cruzi Tulahuen lac-Z strain (IC50 from 7.96 to 21.12 µM), and DBN 1 exhibited the highest activity against the amastigote forms of the T. cruzi Y strain (IC50 3.26 μM). Compounds 1–4 showed CC50 values higher than antitrypanosomal activities, except for DBN 3. All DBNs with antitrypanosomal activity demonstrated CH50 higher than 100 µM. The in silico results indicated that DBNs 1, 2, and 4 are capable of destabilizing the dynamics of the tubulin-microtubule from the vinca site. These compounds displayed promising in vitro activity against T. cruzi, especially compound 1, and can be considered molecular prototypes for the development of new antiparasitic drugs.
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41

Szabó, Lara U., Marcel Kaiser, Pascal Mäser, and Thomas J. Schmidt. "Antiprotozoal Nor-Triterpene Alkaloids from Buxus sempervirens L." Antibiotics 10, no. 6 (June 10, 2021): 696. http://dx.doi.org/10.3390/antibiotics10060696.

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Malaria and human African trypanosomiasis (HAT; sleeping sickness) are life-threatening tropical diseases caused by protozoan parasites. Due to limited therapeutic options, there is a compelling need for new antiprotozoal agents. In a previous study, O-tigloylcyclovirobuxeine-B was recovered from a B. sempervirens L. (common box; Buxaceae) leaf extract by bioactivity-guided isolation. This nor-cycloartane alkaloid was identified as possessing strong and selective in vitro activity against the causative agent of malaria tropica, Plasmodium falciparum (Pf). The purpose of this study is the isolation of additional alkaloids from B. sempervirens L. to search for further related compounds with strong antiprotozoal activity. In conclusion, 25 alkaloids were obtained from B. sempervirens L., including eight new natural products and one compound first described for this plant. The structure elucidation was accomplished by UHPLC/+ESI-QqTOF-MS/MS and NMR spectroscopy. The isolated alkaloids were tested against Pf and Trypanosoma brucei rhodesiense (Tbr), the causative agent of East African sleeping sickness. To assess their selectivity, cytotoxicity against mammalian cells (L6 cell line) was tested as well. Several of the compounds displayed promising in vitro activity against the pathogens in a sub-micromolar range with concurrent high selectivity indices (SI). Consequently, various alkaloids from B. sempervirens L. have the potential to serve as a novel antiprotozoal lead structure.
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42

Abdullahi, Zainab U., Salihu S. Musa, Daihai He, and Umar M. Bello. "Antiprotozoal Effect of Snake Venoms and Their Fractions: A Systematic Review." Pathogens 10, no. 12 (December 16, 2021): 1632. http://dx.doi.org/10.3390/pathogens10121632.

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Background: Protozoal infection is a lingering public health issue of great concern, despite efforts to produce drugs and vaccines against it. Recent breakthrough research has discovered alternative antiprotozoal agents encompassing the use of snake venoms and their components to cure these infections. This study collated the existing literature to examine the antiprotozoal effect of snake venoms and their fractions. Methods: We conducted a systematic review following the PRISMA guidelines. The PubMed and Embase databases were searched from their inception until 13 October 2021. Articles were screened at the title, abstract and full-text phases. Some additional studies were obtained through the manual search process. Results: We identified 331 studies via the electronic database and manual searches, of which 55 reporting the antiprotozoal effect of snake venoms and their components were included in the review. Around 38% of studies examined the effect of whole crude venoms, and a similar percentage evaluated the effect of a proportion of enzymatic phospholipase A2 (PLA2). In particular, this review reports around 36 PLA2 activities and 29 snake crude venom activities. We also report the notable phenomenon of synergism with PLA2 isoforms of Bothrops asper. Importantly, limited attention has been given so far to the antiprotozoal efficacies of metalloproteinase, serine protease and three-finger toxins, although these venom components have been identified as significant components of the dominant venom families. Conclusion: This study highlights the impact of snake venoms and their fractions on controlling protozoal infections and suggests the need to examine further the effectiveness of other venom components, such as metalloproteinase, serine protease and three-finger toxins. Future research questions in this field must be redirected toward synergism in snake venom components, based on pharmacological usage and in the context of toxicology. Ascertaining the effects of snake venoms and their components on other protozoal species that have not yet been studied is imperative.
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43

Ticona, Juan C., Pablo Bilbao-Ramos, Ángel Amesty, Ninoska Flores, M. Auxiliadora Dea-Ayuela, Isabel L. Bazzocchi, and Ignacio A. Jiménez. "Flavonoids from Piper Species as Promising Antiprotozoal Agents against Giardia intestinalis. Structure-Activity Relationship and Drug-Likeness Studies." Pharmaceuticals 15, no. 11 (November 10, 2022): 1386. http://dx.doi.org/10.3390/ph15111386.

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Diarrhea diseases caused by the intestinal protozoan parasite Giardia intestinalis are a major global health burden. Moreover, there is an ongoing need for novel anti-Giardia drugs due to drawbacks with currently available treatments. This paper reports on the isolation and structural elucidation of six new flavonoids (1–6), along with twenty-three known ones (7–29) from the Piper species. Their structures were established by spectroscopic and spectrometric techniques. Flavonoids were tested for in vitro antiprotozoal activity against Giardia intestinalis trophozoites. In addition, structure-activity relationship (SAR) and in silico ADME studies were performed to understand the pharmacophore and pharmacokinetic properties of these natural compounds. Eight flavonoids from this series exhibited remarkable activity in the micromolar range. Moreover, compound 4 was identified as having a 40-fold greater antiparasitic effect (IC50 61.0 nM) than the clinical reference drug, metronidazole (IC50 2.5 µM). This antiprotozoal potency was coupled with an excellent selectivity index (SI 233) on murine macrophages and in silico drug-likeness. SAR studies revealed that the substitution patterns, type of functional group, and flavonoid skeleton played an essential role in the activity. These findings highlight flavonoid 4 as a promising candidate to develop new drugs for the treatment of Giardia infections.
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Żwawiak, Justyna, Dorota Olender, and Lucjusz Zaprutko. "Some nitroimidazole derivatives as antibacterial and antifungal agents in in vitro study." Journal of Medical Science 88, no. 1 (March 30, 2019): 47–51. http://dx.doi.org/10.20883/jms.218.

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Nitroimidazoles have wide range of therapeutic uses mainly as anaerobic antibacterials and antiprotozoal agents. Some bicyclic nitroimidazodihydrooxazoles and nitroimidazotetrahydrooxazines are found to be antituberculosis agents. Hence, the biological and chemical properties of mentioned substances are of great interest to scientists. The aim of this review is to show the general knowledge concerning the chemistry and biological activity of some nitroimidazole derivatives, based on experimental studies. The results of biological tests provide many useful information on the effects of particular groups or other structural elements on the level of pharmacological activity. Also, these studies can be helpful in further planning of syntheses of active substances with using nitroimidazole moiety.
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SALEH, MONA, ABDEL-AZEEM ABDEL-BAKI, MOHAMED A. DKHIL, MANSOUR EL-MATBOULI, and SALEH AL-QURAISHY. "Antiprotozoal effects of metal nanoparticles against Ichthyophthirius multifiliis." Parasitology 144, no. 13 (July 12, 2017): 1802–10. http://dx.doi.org/10.1017/s0031182017001184.

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SUMMARYIchthyophthirius multifiliis is a widespread, ciliated protozoan ectoparasite of fish. In the present study, we investigated the effects of metal nanoparticles on the reproduction and infectivity of free-living stages of I. multifiliis. We determined that ~50% of theronts could be killed within 30 min of exposure to either 20 ng mL−1 gold, 10 ng mL−1 silver or 5 ng mL−1 zinc oxide nanoparticles. Silver and zinc oxide nanoparticles at concentration of 10 and 5 ng mL−1 killed 100 and 97% of theronts, respectively and inhibited reproduction of tomonts after 2 h exposure. Gold nanoparticles at 20 ng mL killed 80 and 78% of tomonts and theronts 2 h post exposure, respectively. In vivo exposure studies using rainbow trout (Oncoryhnchus mykiss) demonstrated that theronts, which survived zinc oxide nanoparticles exposure, showed reduced infectivity compared with control theronts. No mortalities were recorded in the fish groups cohabited with theronts exposed to either nanoparticles compared with 100% mortality in the control group. On the basis of the results obtained from this study, metal nanoparticles particularly silver nanoparticles hold the best promise for the development of effective antiprotozoal agents useful in the management of ichthyophthiriosis in aquaculture.
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46

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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47

Sierra, Elkin Jose Torres, Cleydson Finotti Cordeiro, Livia de Figueiredo Diniz, Ivo Santana Caldas, Jamie Anthony Hawkes, and Diogo Teixeira Carvalho. "Correction to: Coumarins as Potential Antiprotozoal Agents: Biological Activities and Mechanism of Action." Revista Brasileira de Farmacognosia 32, no. 1 (October 18, 2021): 144. http://dx.doi.org/10.1007/s43450-021-00188-9.

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48

Colletti, Steven L., Chunshi Li, Michael H. Fisher, Matthew J. Wyvratt, and Peter T. Meinke. "Tryptophan-replacement and indole-modified apicidins: synthesis of potent and selective antiprotozoal agents." Tetrahedron Letters 41, no. 41 (October 2000): 7825–29. http://dx.doi.org/10.1016/s0040-4039(00)01363-0.

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49

Saccoliti, Francesco, Valentina Noemi Madia, Valeria Tudino, Alessandro De Leo, Luca Pescatori, Antonella Messore, Daniela De Vita, et al. "Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents." European Journal of Medicinal Chemistry 156 (August 2018): 53–60. http://dx.doi.org/10.1016/j.ejmech.2018.06.063.

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50

Arafa, Reem K., Mohamed A. Ismail, Manoj Munde, W. David Wilson, Tanja Wenzler, Reto Brun, and David W. Boykin. "Novel linear triaryl guanidines, N-substituted guanidines and potential prodrugs as antiprotozoal agents." European Journal of Medicinal Chemistry 43, no. 12 (December 2008): 2901–8. http://dx.doi.org/10.1016/j.ejmech.2008.02.008.

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