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 38 for “"antiparasitic"”.
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SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL ANTIPARASITIC AND ANTICANCER AGENTS
… acid derivatives, which have demonstrated antiparasitic properties. These moieties were linked through different molecular connectors to optimize pharmacological properties and evaluated for their activity against Trypanosoma brucei and Leishmania species, with the most potent compound …
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Engagement of human host receptors by the antiparasitic drug praziquantel
… PZQ is necessary to aid the development of new antiparasitic therapies and provide treatment alternatives in face of the threat of drug resistance. One obstacle has been the difficulty of heterologously expressing parasite proteins to profile their drug sensitivity. Consequently, I have taken …
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Utilization of the Baylis-Hillman and related reactions in antiparasitic drug discovery
… utilized extensively in the search for antiparasitic agents. Work in this dissertation describes a series of compounds based on the Baylis-Hillman and the related three-component aza Baylis-Hillman reactions synthesised for biological evaluation as potential inhibitors of two parasitic …
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New mono and bimetallic chloroquine derivatives : synthesis and evaluation as antiparasitic agents
Several series of new ferrocenyl-quinoline antimalarial agents have been synthesised and fully characterised using standard spectroscopic and analytical techniques. The molecular structure of N-(7-Chloro-quinolin-4-yl)-N'-[2 -( N”,N""-dimethylaminomethyl)ferrocenylmethyl]-ethane-1.2-diamine has …
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Synthesis and biological evaluation of antiparasitic Cysteine protease inhibitors based on the Isatin Scaffold
Widespread drug resistance, loss of efficacy and toxicity has limited the full utilization of the current available drugs against malaria and other parasitic diseases. This necessitates the development of new drugs. Meanwhile, the cysteine protease family of enzymes has been identified as potential …
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Development of organosilane-containing bioorganometallic compounds evaluated as antiparasitic agents against Plasmodium falciparum and Trichomonas vaginalis
Many successful initiatives have been employed to stem the spread of the diseases such as malaria and trichomonas's. However, in cases where infection has occurred, pharmaceutical treatments are required. A problem seen across the board is the development of resistance to known treatments. An even …
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The Synthesis of Functionalized Glycosides: Coordination Chemistry, Antiparasitic Activity, Precursors to Conformationally Constrained Macrocyclic Architectures and Photophysical Properties
… to form metal complexes and the study of the antiparasitic activity of both the free glycosides and metal complexes, the use of glycosides to serve as precursors to conformationally constrained macrocyclic molecules and a preliminary investigation of the photophysical properties of a …
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Synthesis, structure-activity relationship and solubility improvement studies of potential antimalarial and antischistosomal pyrido[1,2-a]benzimidazoles
… Recently, Mayoka reported the impressive dual antiparasitic potency of the lead compound GMP-19 (figure 1) against Plasmodium and Schistosoma parasites in vitro (IC50 = 0.430 μΜ, drug sensitive strain (NF54) and IC50 = 0.210 μΜ, adult S. mansoni, (unpublished data)). However, GMP-19 and other …
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Antileishmania Compounds From An Unidentified Endophytic Fungus And Biotransformation Of 5,7,2`,4`,5`-Pentahydroxyflavonol
… from endophytic fungi have been screened for antiparasitic activity against Leishmania donovani and Plasmodium falciparum. The active samples were further evaluated regarding their toxicity versus mammalian cell lines. From the results, DC401 was identified as a promising source of new …
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Synthesis of pyrrolo[2,3-d]pyrimidines and pyrazino[2,3-d]pyrimidines and their biological activities
… to good yields. Cytotoxic, antibacterial and antiparasitic activities were screened for thirty pteridines and eight 7-deazapurines. In many cases, pteridines having 2-chlorophenyl groups at C6 and C7 exhibited cell growth inhibition for cancer/normal cells and bacterial cells. The majority of …
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Modular Synthesis and Hydroalkylation of Vicinally Functionalized Ketopiperazines: A solution to the Piperazine Problem
… biological activities such as antidepressant, antiparasitic, anticancer and antiretroviral. Current methods towards functionalized piperazines include intramolecular cyclization of appropriately tethered on acyclic precursors as well as α-C–H functionalization of intact piperazine rings. …
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New therapeutic strategies against trypanosomiasis and leishmaniasis
… order to investigate the possible mechanism of antiparasitic action of the compounds, this study employed flow cytometry to assess the mitochondrial membrane potential m, as well as parameters such as production of reactive oxygen species (ROS), the permeability of the plasma membrane and any …
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Multidimensional profiling of the Toxoplasma gondii proteome
… proteome profiling to identify the target of an antiparasitic compound, thereby enhancing our understanding of parasite calcium signaling pathways. In a conceptual leap, I applied this method to systematically identify calcium-responsive proteins on the basis of biochemical interactions with this …
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Friends or foes? Blood parasite costs and defence abilities in young raptor hosts
… show that nestlings already possess functional antiparasitic defences. This may provide the opportunity for growing hosts to rely on moderate defence responses, sometimes leading to disease symptoms during the harshest of infections and potentially impairing fitness of some particularly …
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Identification and characterization novel of cystine-loop ligand- gated chloride channels from Dirofilaria immitis: pharmacological analysis and novel compound screening
… LGC-47. Additionally, novel derivatives of the antiparasitic drug levamisole were tested on ACC receptors to determine if any modifications enhanced levamisole action. D. immitis UNC-49B assembled as a homomeric channel and exhibited an EC50 of 5mM for GABA. UNC-49B also formed a functional …
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The Bioactivity and Natural Products of Scottish Seaweeds
… human health. Ethyl acetate extracts showed high antiparasitic activity against Trypanosoma brucei with a P. fucoides extract showing antibacterial activity toward Staphylococcus aureus. Extracts of H. siliquosa and F. serratus showed cytotoxicity to<br/>Hela cells with extracts of H. siliquosa …
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Lipid Targets of the Antimalarial Trioxanes in <i>Plasmodium falciparum</i>
… and therefore may be crucial to their antiparasitic mechanism.</p>
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Benzannulated indoles as drug discovery templates. Efforts towards the total synthesis of a library of therapeutic candidates inspired by Cis-Trikentrin A
… have demonstrated promising anticancer, antiparasitic, and analgesic activity. Additionally, several key intermediates in the synthetic route towards these libraries have demonstrated newly discovered therapeutic value for a rare and aggressive cancer, sinonasal undifferentiated carcinoma …
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Synthesis of the Natural Alkaloids Angustureine, Cuspareine, Galipeine, Galipinine using α-Aminocycloalkyl Copper Reagents
… medications including antibacterial and antiparasitic drugs. The Hancock alkaloids, Galipinine, Galipeine, Cuspareine and Angustureine, are natural 1,2,3,4- tetrahydroquinoline compounds that are found in the South American Angostura tree. Extracts containing these alkaloids have been …
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The Novel Long Non-Coding RNA Nostrill Regulates Intestinal Epithelial Defense Against Cryptosporidium parvum and Modulates Microglial-Mediated Neurotoxicity
… of Nostrill promotes intestinal epithelial antiparasitic defense against C. parvum through contributions to transcriptional regulation of immune-related genes, such as Irf7, and may provide a novel therapeutic target to enhance treatment of cryptosporidiosis. LncRNAs may help direct …
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