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 22 for “"ADME"”.
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Development of in silico models for the prediction of toxicity incorporating ADME information
… distribution, metabolism and elimination (ADME) parameters with an emphasis on absorption and xenobiotic metabolism. These two ADME properties largely determine bioavailability of a drug and, in turn, also influence toxicity. In vitro (Caco-2 cells and the parallel artificial membrane …
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Nash Alters Drug Metabolizing Enzyme and Transporter Expression Resulting in Significant Consequences for Pharmaceutical Disposition and Toxicity
… of removal is a collection of processes known as ADME (absorption, distribution, metabolism, and excretion). The dynamics of ADME ultimately determine the fate, or pharmacokinetics, of a xenobiotic in the body whether it be an administered pharmaceutical or a potentially harmful toxicant. The …
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Pharmacogenetic analysis of admc polymorphisms affecting the efficacy of TB treatment in tuberculosis patients from Tanzania and Uganda, and pharmalogical evaluation of potent medicinal plant extracts used in the treatment of tuberculosis
… anti-TB drugs may also depend on an individual's ADME polymorphisms. Aim: This study was aimed at evaluating the pharmacogenetics of Tanzanian and Ugandan tuberculosis patients, and pharmacological effects of medicinal plants [S. brachypetala (MMV004), R. caffra (MMV003), S. molle (MMV005), Z. …
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The design, synthesis, and biological evaluation of aplysinopsin analogs as potential neuromodulators
… of aplysinopsin analogs, we used an in silico ADME predictor (QikProp) to evaluate and design a new series of analogs with improved ADME properties. We also evaluated the metabolic stability of compound 53 and found that the aplysinopsin scaffold does not appear to be overly susceptible to …
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Drug discovery at the site of pulmonary tuberculosis
… distribution, metabolism, and excretion (ADME) assays were performed to predict the abilities of the compounds to penetrate different TB microenvironments. Penetration into murine blood and organs was assessed via pharmacokinetic (PK) profiling. Complementary analyses involving murine …
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Investigating the nuclear import protein KPn߀1 as a cancer therapeutic target
… associated with Kpnβ1, (iii) its in vitro ADME pharmacokinetics and in vivo anti-cancer properties and (iv) performing biophysical analysis of Kpnβ1:C60 interactions. Cervical and oesophageal cancer cells were found to be more sensitive to C60 treatment compared to non-cancer epithelial …
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Characterising the anticancer effects of a small molecule with potential to inhibit nuclear import via karyopherin beta1
… behaviour of C53 in a living system, in vitro ADME pharmacokinetic studies showed that C53 has moderate solubility, permeability and protein binding however, rapid clearance was shown by liver microsome assay. In vivo repeated dose toxicology studies showed that C53 is tolerable in nude mice. …
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Técnicas de aprendizaje automático y computación científica aplicadas a la predicción de parámetros ADMET-Tox
… de su desarrollo debido al comportamiento ADME-Tox. Por estos motivos, el interes en la industria y el ambito academico en las disciplinas de quimioinformatica y, en particular, en las tecnicas de tipo QSAR ha crecido considerablemente en los ultimos a~nos. El objetivo de esta tesis se …
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The Discovery and Development of Thienopyrimidines as Inhibitors of Helicobacter pylori
… to discover novel scaffolds with improved ADME properties. The pyrrolopyrimidine 56 emerged with good anti-H. pylori activity, an improved solubility and is less bound to human plasma protein. Lead optimization efforts are ongoing, to realize proof of concept of this series of compounds in …
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Optimizing pharmacokinetic studies utilizing microsampling
… distribution, metabolism and excretion (ADME) of an externally administered compound within the body. This is done by measuring the concentration of the compound in some form of bodily tissue (such as whole blood or plasma) at a number of time points after administration. There are two …
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Effects of Febuxostat on Autistic Behaviors and Computational Investigations of Diffusion and Pharmacokinetics
… no literature surrounding tissue and organ ADME for febuxostat the final proposed model would need to be updated as new information becomes available.
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The Design and Synthesis of β-Keto Vinyl Sultams and Macrocyclic β-Keto Vinyl Sultams: Novel Analogs of Tetramic Acids
… to modulate biological activity as well as ADME profiles of the resulting analogs compounds. This thesis will describe the design and synthesis of β-keto sultam analogs of tetramic acids and their corresponding unsaturated and macrocyclic derivatives as novel electrophilic probes that can be …
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Hear Today, Gone Tomorrow: Exploring Quinoxaline Derivatives as a Treatment for Noise-Induced Hearing Loss
… bioavailability was assessed using an in silico ADME assay from SwissADME. A kinome activity assay was performed on organs of Corti to assess changes in kinase activity following noise exposure. We found that Qx34 and Qx62 had the most beneficial effects on noise-exposed animals; they recovered …
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GDGT liposomes for oral peptide delivery
… κατανομής, μεταβολισμού και αποβολής (ADME) αρχαιοβακτηριακών λιπιδίων έπειτα από από του στόματος χορήγηση. Για την υποστήριξη αυτού του ευρύτερου στόχου, χρησιμοποιήθηκε ως πρότυπο σύστημα η οκτρεοτίδη ενθυλακωμένη σε αρχαιοσώματα, προκειμένου να μελετηθούν τόσο η συμπεριφορά των …
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Design, Synthesis, and Evaluation of Novel Antimycobacterial Agents With Enhanced Pharmacokinetic Profiles
… compared to indoles, while maintaining optimal ADME-Tox.
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The characterization of pharmacokinetic properties and evaluation of in vitro drug combination efficacies of novel antimalarial compounds
… distribution, metabolism, and elimination (ADME) properties of the compounds were also determined through the application of specific assays. In vivo pharmacokinetic (PK) profiling was also carried out by intravenous and oral administration of the individual compounds to healthy C57BL/6 …
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Optimization of Quinone-Based, Extracellular Electron Transfer Mediators for Bioelectronic Applications
… based on in vivo data, molecular modeling, and ADME properties of all mediators. Lastly, highly active EET amine-substituted 1,4-naphthoquionones are proposed to be covalently bound to polymer networks. The redox-active polymers are to be embedded on an electrode for the purposes of enhancing …
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Antimalarial Agents: New Mechanisms of Actions for Old and New Drugs
… confirming that they target the MEP pathway. ADME-Tox evaluation of these new analogs will soon be underway.
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Caratterizzazione del legame di molecole di interesse farmaceutico alla sieroalbumina umana mediante biocromatografia e dicroismo circolare
… che permettessero di caratterizzare le proprietà ADMET dei farmaci in via di sviluppo, il più rapidamente possibile. Questa tendenza origina dalla consapevolezza che circa la metà dei farmaci in via di sviluppo non viene commercializzato perché ha carenze nelle caratteristiche ADME, e che almeno …
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Pharmaceuticals in the Environment: Assessing Potential Risks to Fish
The widespread presence of human pharmaceuticals in aquatic ecosystems potentially poses a significant threat to vulnerable organisms, such as fish. To address this issue, the environmental risk assessment (ERA) of active pharmaceutical ingredients (APIs) is now integrated into various regulatory …
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