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Journal articles on the topic 'Schizonticide activity'

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1

Andersen, S. L., P. McGreevy, B. G. Schuster, et al. "Activity of Azithromycin as a Blood Schizonticide against Rodent and Human Plasmodia In Vivo." American Journal of Tropical Medicine and Hygiene 52, no. 2 (1995): 159–61. http://dx.doi.org/10.4269/ajtmh.1995.52.159.

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2

Fonte, Mélanie, Natália Tassi, Paula Gomes, and Cátia Teixeira. "Acridine-Based Antimalarials—From the Very First Synthetic Antimalarial to Recent Developments." Molecules 26, no. 3 (2021): 600. http://dx.doi.org/10.3390/molecules26030600.

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Malaria is among the deadliest infectious diseases in the world caused by Plasmodium parasites. Due to the high complexity of the parasite’s life cycle, we partly depend on antimalarial drugs to fight this disease. However, the emergence of resistance, mainly by Plasmodium falciparum, has dethroned most of the antimalarials developed to date. Given recent reports of resistance to artemisinin combination therapies, first-line treatment currently recommended by the World Health Organization, in Western Cambodia and across the Greater Mekong sub-region, it seems very likely that artemisinin and i
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3

Ferrara, Luciana, and Srinivas G. "Bioequivalence of two quinidine gluconate 324mg extended release formulations in healthy Brazilian volunteers under fed conditions: a pilot study." International Journal of Basic & Clinical Pharmacology 7, no. 7 (2018): 1238. http://dx.doi.org/10.18203/2319-2003.ijbcp20182405.

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Background: Quinidine is an antimalarial schizonticide and an antiarrhythmic agent with Class Ia activity. The present study was aimed at analyzing the bioequivalence of the proposed generic product Quinidine Gluconate 324mg Extended Release Tablets with the marketed product of Sun pharmaceuticals, USA.Methods: The design was an open, longitudinal, randomized, comparative study of two formulations in single dose of 324 mg, with a 5 days washout in between doses. The study was conducted in 12 healthy adult male and female Brazilian volunteers under fed conditions in Azidus Brasil, Valinhos, Bra
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4

Birrell, Geoffrey W., Matthew P. Challis, Amanda De Paoli, et al. "Multi-omic Characterization of the Mode of Action of a Potent New Antimalarial Compound, JPC-3210, Against Plasmodium falciparum." Molecular & Cellular Proteomics 19, no. 2 (2019): 308–25. http://dx.doi.org/10.1074/mcp.ra119.001797.

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The increasing incidence of antimalarial drug resistance to the first-line artemisinin combination therapies underpins an urgent need for new antimalarial drugs, ideally with a novel mode of action. The recently developed 2-aminomethylphenol, JPC-3210, (MMV 892646) is an erythrocytic schizonticide with potent in vitro antimalarial activity against multidrug-resistant Plasmodium falciparum lines, low cytotoxicity, potent in vivo efficacy against murine malaria, and favorable preclinical pharmacokinetics including a lengthy plasma elimination half-life. To investigate the impact of JPC-3210 on b
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5

Dow, Geoffreym S., James A. Reynoldson, and R. C. Andrew Thompson. "Plasmodium berghei: A New Rat Model for Assessment of Blood Schizonticidal Activity." Experimental Parasitology 93, no. 2 (1999): 92–94. http://dx.doi.org/10.1006/expr.1999.4433.

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6

Tan-ariya, P., K. Na-Bangchang, R. Ubalee, S. Boutes, S. Riengchainam, and J. Karbwang. "In vitro blood schizonticidal activity of sera containing mefloquine-quinine against Plasmodium falciparum." Tropical Medicine and International Health 2, no. 2 (1997): 159–64. http://dx.doi.org/10.1046/j.1365-3156.1997.d01-243.x.

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7

Kuhen, Kelli L., Arnab K. Chatterjee, Matthias Rottmann, et al. "KAF156 Is an Antimalarial Clinical Candidate with Potential for Use in Prophylaxis, Treatment, and Prevention of Disease Transmission." Antimicrobial Agents and Chemotherapy 58, no. 9 (2014): 5060–67. http://dx.doi.org/10.1128/aac.02727-13.

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ABSTRACTRenewed global efforts toward malaria eradication have highlighted the need for novel antimalarial agents with activity against multiple stages of the parasite life cycle. We have previously reported the discovery of a novel class of antimalarial compounds in the imidazolopiperazine series that have activity in the prevention and treatment of blood stage infection in a mouse model of malaria. Consistent with the previously reported activity profile of this series, the clinical candidate KAF156 shows blood schizonticidal activity with 50% inhibitory concentrations of 6 to 17.4 nM agains
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8

Ezedom, Theresa, Olukemi Opajobi, Innocent Onyesom, and Lilian Chris-Ozoko. "Blood Schizonticidal Activity of Phyllanthus amarus Enhances Testovarian Antioxidant Defense Capacity in Plasmodium berghei Infected Mice." Tropical Journal of Natural Product Research 2, no. 3 (2018): 150–57. http://dx.doi.org/10.26538/tjnpr/v2i3.10.

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9

Belay, Wubetu Yihunie, Abyot Endale Gurmu, and Zewdu Birhanu Wubneh. "Antimalarial Activity of Stem Bark of Periploca linearifolia during Early and Established Plasmodium Infection in Mice." Evidence-Based Complementary and Alternative Medicine 2018 (2018): 1–7. http://dx.doi.org/10.1155/2018/4169397.

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Background. In Ethiopia, stem bark of Periploca linearifolia is used for the treatment of malaria by the local community and demonstrated antimalarial activity in vitro. Despite its in vitro antimalarial activity, no scientific study has been carried out to verify its activity in vivo. Therefore, the aim of the study was to evaluate the antimalarial activity of Periploca linearifolia stem bark extract in mice. Methods. The dried stem bark of Periploca linearifolia was extracted with 80% methanol and evaluated for its antimalarial activity on both early and established Plasmodium berghei infect
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10

Osunkwo, UA, GC Akuodor, Maryam Idris-Usman, TheresaC Ugwu, JL Akpan, and SI Ghasi. "In vivo schizonticidal activity of ethanolic leaf extract of gongronema latifolium on plasmodium berghei berghei in mice." Ibnosina Journal of Medicine and Biomedical Sciences 2, no. 3 (2010): 118. http://dx.doi.org/10.4103/1947-489x.210981.

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11

SMITH, PAUL W., THIERRY T. DIAGANA, and BRYAN K. S. YEUNG. "Progressing the global antimalarial portfolio: finding drugs which target multiple Plasmodium life stages." Parasitology 141, no. 1 (2013): 66–76. http://dx.doi.org/10.1017/s0031182013000747.

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SUMMARYThe number of novel antimalarial candidates entering preclinical development has seen an increase over the last several years. Most of these drug candidates were originally identified as hits coming from screening large chemical libraries specifically targeting the asexual blood stages of Plasmodium falciparum. Indeed, a large proportion of the current antimalarial arsenal has mainly targeted the asexual blood stage which is responsible for clinical symptoms of the disease. However, as part of the eradication agenda and to address resistance, any next-generation antimalarial should have
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12

Young, R. D., and P. K. Rathod. "Clonal viability measurements on Plasmodium falciparum to assess in vitro schizonticidal activity of leupeptin, chloroquine, and 5-fluoroorotate." Antimicrobial Agents and Chemotherapy 37, no. 5 (1993): 1102–7. http://dx.doi.org/10.1128/aac.37.5.1102.

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13

Echezona, Adaeze Chidiebere, Mumuni Momoh, Paul Achile Akpa, et al. "Effect of molecular interaction on the antiplasmodial efficacy of lumefantrine in amorphous polymethacrylate-urea solid solution." Journal of Drug Delivery and Therapeutics 10, no. 5 (2020): 56–69. http://dx.doi.org/10.22270/jddt.v10i5.4279.

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Malaria, a leading cause of mortality and morbidity in the developing world, with children aged under 5 years, accounts for 61% of all the global malaria deaths. The World Health Organization approved fixed-dose first-line artemisinin-based combination therapy (ACT) – artemether-lumefantrine for effective malaria treatment, is challenged by poor aqueous solubility and inadequate bioavailability leading to treatment failures and emergence of resistant strains. This study focuses on evaluating novel lumefantrine (LF) polymethacrylate-urea solid solutions comprising of a retarding polymer for enh
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14

McCarthy, James S., Bryan Smith, Mark Reid, et al. "Blood Schizonticidal Activity and Safety of Tafenoquine When Administered as Chemoprophylaxis to Healthy, Nonimmune Participants Followed by Blood Stage Plasmodium falciparum Challenge: A Randomized, Double-blind, Placebo-controlled Phase 1b Study." Clinical Infectious Diseases 69, no. 3 (2018): 480–86. http://dx.doi.org/10.1093/cid/ciy939.

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Abstract Background Tafenoquine was recently approved for chemoprophylaxis of malaria. Its specific activity against liver and blood stages of Plasmodium species has been separately characterized in animals but not in humans. Methods In this randomized, double-blind, placebo-controlled study, 16 malaria-naive, glucose-6-phosphate dehydrogenase–normal participants aged 20–42 years received tafenoquine chemoprophylaxis prior to challenge with blood stage Plasmodium falciparum. Participants were randomly assigned to either tafenoquine (n = 12) or placebo (n = 4) and took blinded study medication
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15

Dola, Vasantha Rao, Awakash Soni, Pooja Agarwal, et al. "Synthesis and Evaluation of Chirally Defined Side Chain Variants of 7-Chloro-4-Aminoquinoline To Overcome Drug Resistance in Malaria Chemotherapy." Antimicrobial Agents and Chemotherapy 61, no. 3 (2016). http://dx.doi.org/10.1128/aac.01152-16.

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ABSTRACT A novel 4-aminoquinoline derivative [(S)-7-chloro-N-(4-methyl-1-(4-methylpiperazin-1-yl)pentan-2-yl)-quinolin-4-amine triphosphate] exhibiting curative activity against chloroquine-resistant malaria parasites has been identified for preclinical development as a blood schizonticidal agent. The lead molecule selected after detailed structure-activity relationship (SAR) studies has good solid-state properties and promising activity against in vitro and in vivo experimental malaria models. The in vitro absorption, distribution, metabolism, and excretion (ADME) parameters indicate a favora
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16

Wadi, Ishan, Pargat Singh, Mahendra Nath, Anupkumar R. Anvikar, and Abhinav Sinha. "Malaria transmission-blocking drugs: implications and future perspectives." Future Medicinal Chemistry, May 7, 2020. http://dx.doi.org/10.4155/fmc-2020-0026.

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Since the world is inching toward malaria elimination, the scientific community worldwide has begun to realize the importance of malaria transmission-blocking interventions. The onus of breaking the life cycle of the human malaria parasite Plasmodium falciparum predominantly rests upon transmission-blocking drugs because of emerging resistance to commonly used schizonticides and insecticides. This third part of our review series on malaria transmission-blocking entails transmission-blocking potential of preclinical transmission-blocking antimalarials and other non-malaria drugs/experimental co
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17

Daher, André, Ghait Aljayyoussi, Dhelio Pereira, et al. "Pharmacokinetics/pharmacodynamics of chloroquine and artemisinin-based combination therapy with primaquine." Malaria Journal 18, no. 1 (2019). http://dx.doi.org/10.1186/s12936-019-2950-4.

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Abstract Background Activation of hypnozoites of vivax malaria causes multiple clinical relapses, which contribute to the Plasmodium vivax burden and continuing transmission. Artemisinin-based combination therapy (ACT) is effective against blood-stage P. vivax but requires co-administration with primaquine to achieve radical cure. The therapeutic efficacy of primaquine depends on the generation of a therapeutically active metabolite via cytochrome P450 2D6 (CYP2D6). Impaired CYP2D6 metabolism has been associated with primaquine treatment failure. This study investigated the association between
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18

Dow, Geoffrey, and Bryan Smith. "The blood schizonticidal activity of tafenoquine makes an essential contribution to its prophylactic efficacy in nonimmune subjects at the intended dose (200 mg)." Malaria Journal 16, no. 1 (2017). http://dx.doi.org/10.1186/s12936-017-1862-4.

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