Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 86 for “"antimalarials"”.
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Antimalarials from Plant Pathogenic Fungi
The purpose of this study was to discover antimalarial compounds from necrotropic plant pathogenic fungi. Various phytotoxins released by necrotropic plant pathogenic fungi may inhibit the plant-like metabolic pathways in the apicoplast, a chloroplast-like organelle, essential for the survival of …
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Investigating calcium channel blockers as antimalarials
… further as a combinatory partner with other antimalarials, and as a scaffold to synthesise other potentially more potent fendiline analogues.
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Antimalarials based on the arylpiperazine privileged substructure
Based on a previous study, arylpiperazines (2-chlorophenylpiperazine, 2-ethoxyphenylpiperazine and phenylpiperazine) were found to be significantly more potent against the chloroquine-resistant (K1) strain than against the chloroquine-sensitive(DIO) strain. In other studies, …
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Antitumor activity of antimalarials in human breast cancer cells
… and apoptosis is generalizable to quinoline antimalarials, we tested typical quinoline antimalarial drugs for their ability to regulate MCF-7 cell differentiation, hyperacetylation histone H4 and apoptosis. MTS IC50 of amodiaquin, chloroquine, primaquine, quinidine as well as quinine induced …
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Discovery, Isolation, and Identification of Antimalarials from Fungal Endophytes
We examined fungal endophytes for their ability to inhibit bacterial, fungal and protozoal pathogens. Once antimalarial activity was discovered and confirmed, we sought to isolate and identify the active constituent(s) of our extracts. Bioassay-guided fractionation techniques were used to isolate …
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Hit to Lead Stage Optimization of Orally Efficacious β-Carboline Antimalarials
… of the stereoisomers of TCMDC-140230 were potent antimalarials (IC50 = 1,300 – 3,700 nM). However, a significant amount of oxidized byproduct 1-(3,4-dichlorophenyl)-8-methyl-N-(2-(methylamino)ethyl)-9H-pyrido[3,4-b]indole-3-carboxamide (MMV1803522) was observed in the synthesis of (1S,3S)- and …
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Targeting Plasmodium Falciparum Dihydroorotate Dehydrogenase (PfDHODH) for the Development of New Antimalarials
Malaria remains a global health threat, with drug resistance presenting a persistent challenge. Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH), which catalyzes the fourth rate-limiting step of the de novo pyrimidine synthesis, is a validated drug target, yet no inhibitor has surpassed …
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Deconvoluting drug mode-of-action : transcriptomic evaluation of novel clinical lead antimalarials
… the discovery and development of effective antimalarials that target both the proliferative asexual parasite stages and the sexual asymptomatic stages that facilitate transmission to a new host. Furthermore, the immense replicative rate and thus mutational capacity of Plasmodium asexual …
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Investigation of azithromycin analogues and proteasome-like inhibitors as quick-killing antimalarials
… that have severely limited the efficacy of antimalarials, including front-line artemisinins, highlighting the urgent need to identify new antimalarials for use as treatments. The aim of this thesis was to investigate novel antimalarial development avenues and identify new chemotypes that …
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Quantum dot labelled antimalarials and investigation of their interaction with synthetic haemozoin
Chloroquine (CQ) is a well-known antimalarial drug acting through the inhibition of the formation of haemozoin crystals in the Plasmodium parasite’s digestive vacuole within human infected red blood cells. The formation of haemozoin is considered a defence strategy of the parasite in order to …
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Nonclassical Mechanisms to Inhibit β-Hematin Crystallization Illuminate the Cooperative Action of Antimalarials
Malaria parasites survive within red blood cells by converting toxic heme, released during hemoglobin digestion, into inert hemozoin crystals. Because disruption of this detoxification pathway is a major route of parasite killing, understanding how these crystals form and how drugs interfere with …
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Interactions of quinoline antimalarials with haematin and their effect on ß-haematin formation
… compensation in the interaction of quinoline antimalarials with haematin in 40% (v/v) aqueous OMSO has been compared with that in pure aqueous solution. The data indicate that the degree of desolvation and loss of conformational freedom is identical in both systems. The nature of interactions …
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Synthesis and investigation of quinoline based ß-haematin formation inhibitors as potential antimalarials
The question of whether or not replacing the 7-chloro group in the 4-aminoquinoline moiety with an electron withdrawing and hydrophilic substituent results in retention of antiplasmodial activity in the 4-aminoquinoline class of compounds was investigated...
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The role of haem in the mechanism of action of antimalarials in Plasmodium falciparum
… mechanism of action of chloroquine and related antimalarials and several studies have linked inhibition of the formation of synthetic haemozoin, β-haematin, to parasite survival. However, haemozoin inhibition with a dose related increase in "free" haem correlated to decreased survival has not …
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Computational investigation of the Plasmodium falciparum fatty acid biosynthetic pathway toward the discovery of novel antimalarials
The structural peculiarities of a protein are related to its biological function. In the fatty acid elongation cycle, one small carrier protein shuttles and delivers the acyl intermediates from one enzyme to the other. The carrier has to recognize several enzymatic counterparts, specifically …
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The efficacy and safety of artesunate suppositories in combination with other antimalarials in the treatment of severe malaria in Sudan.
… efficacy and safety of three combined antimalarials in preventing recrudescence. The modified HPLC-UV method used in the present study showed appropriate validation and provided accurate characterisation and quantification of artesunate, alpha and beta dihydroartemisinin and artemisinin …
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Insights into the mechanism of action of quinoline antimalarials against Plasmodium falciparum revealed by novel fluorescent analogues and chemical proteomics
… action of the two major classes of the quinoline antimalarials against P. falciparum. These are the quinoline methanols, represented by the diastereomeric Cinchona alkaloids quinine and quinidine, and the 4-aminoquinolines, represented by chloroquine. Mechanistic studies of these antimalarials …
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Totarol as privileged natural product scaffold for antimalarial drug discovery
… A continuous effort to find alternative antimalarials to this drug has led to the discovery of other effective antimalarials of different types, such as aminoquinolines, artemisinins and nucleic acid inhibitors. However, the emergence of multi-drug resistant strains of the malaria …
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