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 10 of 10 for “"Hemozoin"”.
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Synthesis, antimalarial evaluation, Ç-hematin inhibition, and in silico and in vitro ADMET profiling of 4-aminoquinoline-hydroxypyridinone hybrids
… action was studied with respect to inhibition of hemozoin formation.
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Nonclassical Mechanisms to Inhibit β-Hematin Crystallization Illuminate the Cooperative Action of Antimalarials
… 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 their formation is important for both fundamental mechanism and …
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Antimalarial benzimidazoles and related structures incorporating an intramolecular hydrogen bonding motif: medicinal chemistry and mechanistic studies
… lipid bodies that have been implicated in hemozoin formation, it was hypothesized that the parent compounds 1.3 and 3.14 could be inhibiting the formation of hemozoin. Docking studies employed to investigate this hypothesis predicted intermolecular interactions between the parent compounds …
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Mechanism of Action Studies of Phenotypic Whole-cell Active Antimalarial Leads Through Target Identification
… has focused mainly on the inhibition of hemozoin biocrystallization in the acidic digestive vacuole of the parasite. However, the intrinsic fluorescence properties of KP68 and KP124 were used to comprehensively study the subcellular accumulation of these compounds in an infected …
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Characterization of a glycerophosphodiester phosphodiesterase in the human malaria parasite Plasmodium falciparum
… virulence, differentiation, cell-signaling and hemozoin formation. Therefore, investigating enzymes involved in lipid degradation could uncover novel drug targets. We have identified in P. falciparum, a glycerophosphodiester phosphodiesterase (PfGDPD), involved in the downstream pathway of …
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Investigation of Dual Stage Acridones as a Potent Malaria Treatment
… acridones is thought to target heme and inhibit hemozoin formation within the parasite’s digestive vacuole, and is known to provide synergistic effects with other antimalarials such as quinine. Currently, the molecular target(s) of chemotype I acridones are unknown; therefore, we sought to …
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Piperazine-based pyrido[1,2-a]benzimidazoles: synthesis and pharmacological evaluation as potential antimalarial and antischistosomal agents
… activities and their potential to inhibit hemozoin (Hz) formation. This suggests that Hz inhibition is not the sole target of this class of compounds, although it may be a contributory mode of action. Compounds were also screened at 10 µM against newly transformed schistosomula and adult S. …
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Synthesis, biological activity and physicochemical properties evaluation of antiplasmodial pyrimido[1,2-a]benzimidazoles
… compounds were also evaluated in the synthetic hemozoin, beta-hematin inhibition (βHIA) assay. Aqueous solubility, and for selected compounds, microsomal metabolic stability, were also evaluated. The most potent compounds against the asexual blood stage (ABS) parasites belonged to SAR3 series …
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Development of analytical techniques for probing the effects of -haematin inhibiting compounds on the malaria parasite Plasmodium falciparum
… for the study and the design of future hemozoin-inhibiting antimalarial drugs, as well as for our understanding of parasite resistance mechanisms.
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Isolation and characterization of African marine natural products and repositioning of the natural product antibiotic fusidic acid and privileged benzimidazole scaffold for tuberculosis and malaria
… and their likely mode of action as inhibitors of hemozoin formation. The 1-((4-trifluoromethyl)benzyl) benzimidazole analogue based on the 3-((N,N-diethylamino)methyl)-2-hydroxy-5-methyl aniline Mannich base was the most potent analogue in both assays. It recorded a MIC90 value of 2.00 µM in the …