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 45 for “"drug discovery and development"”.
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Xenopus laevis as a chemical genetic screening tool for drug discovery and development.
… chemical genetic screening model towards drug discovery and drug development. The NCI diversity set II compound library was screened to identify abnormal pigmentation generating phenotypes that may have therapeutic application towards the treatment of melanoma cancer. 13 hit compounds …
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Integration of In Silico and In Vitro ADMET properties in lead identification and optimization of compounds for the treatment of parasitic diseases
… infections are the major causes of illness and death in tropical regions especially in Africa. The main parasitic diseases include leishmaniasis, filariasis, malaria, river blindness, Chagas disease and schistosomiasis. With the absence of vaccines, treatment relies mainly on chemotherapy …
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In vitro metabolism of tetrazole aminoquinolines and derivatives of metergoline and fusidic acid
Drug metabolism is recognised as a key component of the drug discovery and development process. It exerts an influence on the action, duration of action and toxicity of a drug in vivo. The integration of drug metabolism studies is therefore crucial to compound progression through the various stages …
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Engineering polymer biomaterial interfaces for promoting cellular morphogenesis
Three-dimensional in vitro tissue and organ cultures have immense promise as models of human pathophysiology and stand to make a significant impact on the process of drug discovery and development. Many existing model systems do not capture the relevant complexity of the native tissue environment, …
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Academia versus industry as a wellspring of new ideas in drug discovery : the case of oncology
The United States population is aging, and the need for novel approaches to treat and manage disease continues to grow. Among the diseases that will impact this population, cancer remains a therapeutic area with significant unmet need. Pharmaceutical and biotechnology industries must continue to …
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Nanocrystallization confined to porous matrices with and without surface functionalization effects
… represent a major fraction of the molecules in drug discovery and development, are a challenge to the pharmaceutical industry given their low bioavailability. One way to address this issue is to generate nanocrystals of these APIs. Nanocrystals have a significantly increased surface area to …
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Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype
… is believed to be a target for most antimalarial drugs. It is in this stage that host haemoglobin is degraded to provide nutrients for the survival of the parasite. However, a pathway (known as the haem detoxification pathway) that gives rise to the unique, microcrystalline ferriprotoporphryin IX …
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Novel Polycyclic Benzannulated Indole Scaffolds via Indole Aryne Cycloaddition, Pd (0)-Catalyzed Cross-coupling and ROM/RCM methodologies: Their Applications to Library Development and Drug Discovery
… is an important element of many natural and synthetic molecules with significant biological activity. Drug discovery and development processes highly value the utility of the ability to synthesize a diverse library based on one core scaffold which can be screened against a variety of …
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A bioactive peptide from the skin secretion of the Chinese Torrent Frog, Amolops wuyiensis
Natural products, as rich and varied resources for the discovery of novel drugs, have been essential for human healthcare systems throughout history. A variety of bioactive components with unique structures and functions which isolated from the skin secretion, especially the peptides, have enormous …
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In-column polymer modifications: Advancing polymer bonded phases
… delivery to cell surface, binding affinity, and mediating different physiological effects. Separations of glycoproteins and their glycoforms are essential for drug discovery and development, identification of potential disease biomarkers and quality control. The efficiency of glycoprotein …
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Pharmacokinetic Evaluation of a Novel Compound, Sn79, a Putative Sigma-2 Receptor Antagonist, By Intravenous and Oral Administration in Rats
Considering the alarming rates at which substance drug abuse, especially cocaine, is increasing in today's society, there is a lot of impetus on the development of medications that can effectively help alleviate its toxicity and addiction. The affinity of cocaine to sigma receptors (sigma-1 and …
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Copper-catalyzed enantioselective stereodivergent synthesis of amino alcohols
… For this reason, it is routine procedure in the drug discovery and development process to prepare the full matrix of possible stereoisomers of drug candidates for biological evaluation and to determine the stereochemical purity of these molecules. Despite many recent advances in asymmetric …
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Business models for information commons in the pharmaceutical industry
… for pharmaceutical firms to invest in developing drugs across a wide variety of major medical needs. However, this traditional drug development process is subject to decreasing productivity and increasing costs. In addition, it encourages pharmaceutical firms to focus on "blockbuster" drugs, and …
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Technological learning and the evolution of the Indian pharmaceutical and biopharmaceutical sectors
The Indian pharmaceutical and biopharmaceutical sectors have been characterised by three features considered analogous to technological stagnation: low R&D investments, "copying" on-patent drugs (legal in India if a novel process is found) and manufacturing off-patent, generic drugs. Yet, some …
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Role of Membrane Transporters in Drug Delivery, Drug Disposition And Drug-Drug Interactions
Tissues such as liver, kidney, brain and intestine expresses membrane transporters which play a vital role in drug absorption, distribution, metabolism and excretion. Understanding of functionality and molecular expression of drug transporters can prove to be of utmost importance in drug delivery …
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Equilibrative Nucleoside Transporter Mediated Drug Disposition Across the Blood-Testis Barrier
… viruses or cancer to persist in the testis, and impedes the development of male contraceptives and fertility treatments. Drug transporters present at the basal and apical membranes of testicular epithelial cells (Sertoli cells) facilitate the disposition of therapeutics across the BTB. Many …
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Intrinsic Flexibility of West Nile Virus Protease: In Solution Characterization
… is a mosquito-borne flavivirus with a rapidly expanding global distribution. Infection can cause severe neurological disease and fatalities in humans. Efforts are ongoing to develop antiviral drugs that inhibit the WNV protease, a viral enzyme required for polyprotein processing. Unfortunately, …
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Molecular recognition from atomic interactions: insights into drug discovery
… industry to increase the delivery of new drugs into the market is driving a re-assessment of practices and methods in drug discovery and development. In particular alternative strategies are being pursued to find therapeutics that are more selective, including small molecules that target …
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Organizational design : the integration of pharmaceutical discovery and development
… failure rates suggesting that targets, leads and clinical candidates may be of lower quality in recent years. Senior R&D management generally believes that a greater integration of drug discovery and development will improve the selection and optimization of clinical candidates. I demonstrate …
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Supramolecular derivatisation of new anti-tubercular and antimalarial drug leads
The UCT Drug Discovery and Design Centre, H3D, provided anti-tubercular and antimalarial drug leads that display potent in vitro and in vivo activity, but with unfavourable physicochemical properties. The primary objective of this study was to prepare supramolecular derivatives of the drug leads in …
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