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 21 for “"antimalarial compounds"”.
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Screening of actinobacteria for novel antimalarial compounds
The success of our first-line antimalarial treatments is threatened by increased drug resistance in Plasmodium parasites. This makes the development of novel drugs critical to combat malaria. Historically, natural products have been an excellent source of novel antimalarial compounds and thus are …
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The design and synthesis of novel potential antimalarial compounds
The work contained in this thesis is split into two sections. Each section covers a different biological pathway, its current importance as a potential drug target, and the syntheses towards a selection of natural products and analogues relevant to the pathway. In Section A, the novel approach …
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Novel Antimalarial Compounds from the Optimization of the Malaria Box
… is of great concern, and the need for novel antimalarial compounds are still urgent. The Malaria Box lead molecules MMV008138 and MMV665831 are promising in this regard, due to their apparently novel antimalarial mechanisms of action. The target of MMV008138 is the PfIspD enzyme in the MEP …
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The characterization of pharmacokinetic properties and evaluation of in vitro drug combination efficacies of novel antimalarial compounds
… difficult. Derivatives of the Chinese peroxidic antimalarial drug artemisinin primarily used in first-line combination therapy for treatment of P. falciparum malaria have proved to be highly effective. However, their use also is now compromised by the development of resistance by the parasite to …
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Multivariate muti-level non-linear mixed-effect models and their application to the modeling of drug-concentration time curves
… concentration-time data for the aforementioned antimalarial compounds, and details the necessary extensions to the basic modeling process that were required in order to accommodate multiple responses and multiple observation phases (pregnant and postpartum).
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Bioactive chloroquine-based ligands and their gold complexes as potential novel antimalarial agents
… have proven to be the most efficacious antimalarial drugs for both the treatment and prophylaxis of malaria. However, with the advent of drug resistance, their ability to treat the disease has been significantly hindered. Future research into the synthesis of new 4-aminoquinoline …
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Directed Evolution of Phosphite Dehydrogenase and Engineered Biosynthesis of Fr-900098
… Phosphonates are a small but growing class of compounds with many useful therapeutic properties. In particular, the phosphonates fosmidomycin and FR-900098 represent a new class of antimalarial compounds that can be used to inhibit the nonmevalonate pathway for isoprenoid biosynthesis in the …
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Computational investigation of the Plasmodium falciparum fatty acid biosynthetic pathway toward the discovery of novel antimalarials
… for the identification of novel pathway-based antimalarial compounds.
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Exploring Protoheme IX Farnesyltransferase as an Antimalarial Drug Target
The search for novel antimalarials continues due to the need to combat the rapidly increasing prevalence of multidrug resistant Plasmodium species parasites that cause malaria. Recent advances in technology to genetically modify malarial parasites and methods for high throughput screening of …
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Toward the synthesis and evaluation of novel N-acylated FR-900098 analogs
… currently at risk. Although there exist several antimalarial drugs to treat the disease, many of them have been used and over-used for decades, leading to widespread resistance in the causative Plasmodium parasite. As a result, new antimalarials are needed not only to replace the old, but also to …
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Proteolysis-targeting chimeras as a novel strategy for targeting epigenetic mechanisms in Plasmodium falciparum parasites
… of resistance to the only remaining effective antimalarial, artemisinin, novel drugs with novel modes-of-action (MoA) are needed. Current antimalarial efforts aim to identify small-molecule inhibitors that bind to the active site of essential target proteins, thereby killing the causative …
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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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Microbial synthesis of antimalarial compound FR-900098: pathway characterization and engineering
… represent a small, but potent group of compounds with many useful therapeutic properties. FR-900098 is a novel chemotherapeutic agent for the treatment of malaria and has been effective in humans and other animals. This compound inhibits 1-deoxy-D-xylulose-5-phosphate (DXP) …
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New approaches for measuring fitness of Plasmodium falciparum mutations implicated in drug resistance
… These were grown in the presence and absence of antimalarial compounds, and growth phenotypes were measured in parallel using BarSeq. The third results chapter studies the contribution of mutations in Pfkelch13, a molecular marker of artemisinin resistance, to parasite fitness. Combining …
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Synthesis and Antimalarial evaluation of Gold Thiosemicarbazone Complexes and Polyamine-Thiosemicarbazone Dendrimers
… on health systems in most affected areas, novel antimalarial compounds are endlessly needed to overcome the problem of malaria infections. This thesis presents research investigating a series of thiosemicarbazones (TSCs) and their novel gold complexes and dendrimers as potential antimalarial …
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New approaches to antimalarial target deconvolution and measuring fitness effects of Plasmodium falciparum mutations implicated in drug resistance.
… resistance is to systematically identify new antimalarials to which the parasite has not yet developed resistance. Many novel compounds with antimalarial activity are in development. However, in most cases, the targets and the mechanisms of action of these compounds are unknown. Understanding …
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The influence of genetic background on drug resistance in the malaria parasite Plasmodium falciparum
… malaria; with multidrug resistance to modern antimalarials emerging and spreading in certain parasite populations, understanding the mechanisms for acquiring multidrug resistance will be key for predicting which genes may become important for clinical resistance in the future. Transporter …
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An in vitro chemogenomic screening system to identify the molecular targets of antimalarial drug candidates
The efficacy of existing antimalarials is threatened by parasite resistance, driving the need for a well-stocked pipeline of potential replacement therapies. A global effort to carry out phenotypic screening in live parasite assays has identified many promising hit compounds, but elucidating the …
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Natural product derivative activates autophagy in cancer cells
… a natural product and its derivatives are potent antimalarial compounds, which have shown anticancer activity. In this study, we further characterized a novel artemisinin derivative namely EXP57EA which was previously designed and synthesized by the Chemistry Department at the University Of Cape …
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Synthesis, biological activity and physicochemical properties evaluation of antiplasmodial pyrimido[1,2-a]benzimidazoles
… has prompted the urgent need to develop new antimalarial drugs with novel modes of action and no cross resistance to existing medicines. Pyrido[1,2-a]benzimidazole (PBI) derivatives have been previously identified as antimalarial compounds with promising in vitro activity against Plasmodium …
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