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 37 for “"Bioactivation"”.
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Bioactivation of diacetyldapsone in cultured lung cells
<p>Dapsone has been shown to be an effective agent against Pneumocystis carinii pneumonia, an opportunistic infection in AIDS patients. Oral administration of dapsone is associated with several adverse effects, including methemoglobinemia, hemolytic anemia and photosensitivity reactions. To reduce …
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BIOACTIVATION OF NATURAL DIETARY PRODRUGS BY SPECIFIC CYTOCHROME P450 ENZYMES
… anticancer prodrugs. This thesis describes the bioactivation of natural prodrugs by tumour specific CYPl enzymes. An initial exploratory investigation was conducted on a variety of natural products including all-/raz7.y-retinoic acid (/-RA), vitamin D3, and the isoflavonoids genistein and …
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Studies on the metabolic bioactivation of haloperidol (HP) and its tetrahydropyridine dehydration product
… if these compounds, like MPTP, undergo metabolic bioactivation to neurotoxic pyridinium metabolites. In vitro metabolic studies have demonstrated that human monoamine oxidase A and cytochrome P450 3A4 are capable of catalyzing the oxidation of HPTP and/or HP to the toxic HP pyridinium metabolite …
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Rational enzyme-directed prodrug development : exploiting tumour hypoxia to target the bioactivation of cytotoxic prodrugs
Conventional cancer chemotherapy often lacks specificity and is consequently associated with significant normal tissue toxicities. Molecular chemotherapy offers the potential to target the activation of inert prodrugs by utilising tumour-specific catalytic enzymes to restrict cytotoxicity to …
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A Bacterial Metabolite Causes Changes in Neurodegeneration and Aging Via Bioactivation and Hormesis in Caenorhabditis Elegans
… revealed neurodegeneration was enhanced through bioactivation of the secondary compound by Phase I and II enzymes, cyp − 35B2. When animals were exposed to this secondary compound at different concentrations, a hormetic aging response was seen. Underlying both phenotypes was the requirement of …
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Investigating the chemical space and metabolic bioactivation of natural products and cross-reactivity of chemical inhibitors in CYP450 phenotyping
… a higher likelihood of undergoing metabolic bioactivation.
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Synthesis and Pulmonary Toxicity of Several 3-Furyl Ketones: Evidence for the Position of Metabolism by Cytochromes P-450
… is of increasing concern to animal science. Bioactivation of these heterocycles by pulmonary cytochromes P-450 is necessary for their toxicity, but the mechanism of this bioactivation is not clearly understood. Using a series of 3-furyl ketone congeners of perilla ketone, …
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Studies on the Synthesis and Rearrangement of Indazolylpyridinium Derivatives Precursors to Potential Neuroprotective Prodrugs Bearing a 1,2,3,6-Tetrahydropyridinyl Carrier
… the monoamine oxidase-B (MAO-B) catalyzed bioactivation of MPTP, the role of nNOS inhibition as a mediator of 7-NI's neuroprotective properties have been challenged. In order to examine in greater detail the neuroprotective effects of indazolyl derivatives, the synthesis of water soluble …
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Investigation into the effects of the tobacco smoke procarcinogen benzo[a]pyrene on gene expression profiles in oesophageal cancer
… genes affect enzyme activity and therefore BaP bioactivation.
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Synthetic and metabolic studies on centrally acting amines
This dissertation is concerned with the metabolic bioactivation of several amines which are either known or suspected to be neurotoxic and with the exploration of bioactivation processes in order to generate metabolites with therapeutic potential. The following three programs were pursued in this …
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Characterizing the Binding Potential, Activity, and Bioaccessibility of Peroxisome Proliferator Activated Receptor Gamma (PPARγ) Ligands in Indoor Dust
… are from indoor dust matrices. In addition, bioactivation of SVOCs (via metabolism) could exacerbate their PPAR potency. Therefore, to adequately assess the potential risk of PPARγ activation from exposure to SVOC mixtures in house dust, it is essential that one also investigates the …
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EFFECTS OF RED BLOOD CELLS ON NITRIC OXIDE BIOACTIVITY
… also can modulate NO export. The nitrite bioactivation in RBCs senses to low oxygen and low nutrients areas. Due to the rate constant of Hb and NO reaction, NO formed in the RBC is not likely to escape scavenging. NO activity is preserved in as a nitrosothiol through a nitrosylation …
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The Role of Ovarian Metabolism in 4-Vinylcyclohexene Metabolites and 7,12-Dimethylbenz[a]anthracene Induced Ovotoxicity in Mice
… 7,12-dimethylbenz[a]anthracene (DMBA) requires bioactivation to induce follicle loss. VCH is bioactivated to monoepoxides (1,2-VCM and 7,8-VCM), and subsequently to an ovotoxic diepoxide (VCD) by hepatic CYP 2A and CYP 2B. DMBA is sequentially bioactivated to the ovotoxicant …
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The plant-activation of m-phenylenediamine and its mutagenic, biochemical and molecular characterization
… biochemical and molecular mechanisms involved in bioactivation of promutagens into mutagens have been partially revealed in mammalian systems to understand cancer induction mechanisms. This laboratory demonstrated that simple aromatic amines are activated into potent frameshift mutagens by …
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Synthesis and MAO activity of a series of benzimidazolyl and indazolyl prodrugs
… compound that releases the enzyme inhibitor upon bioactivation by MAO. These results as well as a MPTP mouse study with the aforementioned compound are detailed within.
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Potential Prodrugs of the Neuronal Nitric Oxide Synthase and Monoamine Oxidase Inhibitor 7-Nitroindazole and Structurally Related Compounds
… release the active drugs following a metabolic bioactivation process. These studies have led to a detailed description of the nucleophilic aromatic substitution reactions between 4-chloro-1-methylpyridinium iodide and the indazolyl reactants that were employed as the initial step in the …
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Microbial glucosinolate metabolism: Characterization of Enterococcus faecalis XL1 and functional analysis of a GH4 enzyme
… insights into how gut bacteria contribute to the bioactivation of dietary GSLs.
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Great Expectations: Phosph(On)Ate Prodrugs In Drug Design—Opportunities and Limitations
… inhibitor prodrugs with diverse mechanisms of bioactivation, and 4.) ongoing efforts to advance the parent nucleoside of remdesivir to the clinic for the treatment of COVID-19. Together, this work epitomizes the necessity of considering model-specific limitations at the in vitro and in vivo …
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