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 68 for “"PHARMACOLOGICAL PROPERTIES"”.
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Microstructural investigation of tablet compaction and tablet pharmacological properties
… and the subsequent impact on tablet properties; this gap presents a barrier to rational formulation / process design. In this study, it was hypothesized that the understanding of tablet microstructure is pivotal in bridging our knowledge about the materials, the manufacturing process, …
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NOVEL STRATEGIES FOR IMPROVING THE PHARMACOLOGICAL PROPERTIES OF PLATINUM-ACRIDINE ANTICANCER AGENTS
… to devise strategies that improve the drug-like properties of platinum-acridines and allow their safe delivery. To achieve this, several classical and newly developed synthetic methodologies have been used to generate functionally unique hybrid agents. Several model systems, whole-cell assays, …
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NOVEL APPROACHES FOR CONTROLLING TARGET SELECTIVITY AND PHARMACOLOGICAL PROPERTIES OF PLATINUM-INTERCALATOR-BASED ANTICANCER AGENTS
… (PK) caused by the poor drug-like properties of these agents. The goal of this dissertation was to devise a structurally minimalistic approach by which platinum-acridines can be tuned to simultaneously achieve both of these goals. In particular, a design was desired that minimizes …
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Investigation of an unusual GABA-A receptor: studies on the promiscuous ε [epsilon] subunit
… subtypes with different, subunit-specific pharmacological properties. GABAA receptors are targeted by many clinically-important drugs, for example, benzodiazepines. Unwanted side effects, such as tolerance and dependence, often occur due to non-selective receptor targeting. There is, …
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The effects of phenylbutazone on a strain of fibroblasts cultivated in vitro
… studied during the previous fifty years, the pharmacological properties were only recently recognized. It has been used clinically since 1952.</p><p>Two other pharmaceutical agents of the pyrazole group are phenazone and amidopyrine; these were used as early as the nineteenth century. While …
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Functional characterisation of aphid, Myzus persicae, nicotinic acetylcholine receptors and identification of a novel biogenic amine-gated ion channel from the honeybee, Apis mellifera
… oocytes, has enabled the study of functional and pharmacological properties of these receptors by two-electrode voltage clamp electrophysiology. Myzus persicae, the peach potato aphid, is a major global pest of multiple crop species. The nAChR subunits and several protein chaperones from Myzus …
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Protein-Ligand Binding Affinity Directed Multi-Objective Drug Design Based on Fragment Representation Methods
… vast molecular space to be explored and numerous pharmacological properties to be appropriately considered. Among various drug design protocols, fragment-based drug design is an effective way of constraining the search space and better utilizing biologically active compounds. Motivated by …
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THE SYNTHESIS, STEREOCHEMISTRY, AND ANTIMICROBIAL PROPERTIES OF SOME SUBSTITUTED CYCLOHEXANE DERIVATIVES AND RELATED ACYCLIC ANALOGUES
… of compounds known to possess a wide range of pharmacological properties, and also an investigation into the stereochemistry and antimicrobial properties of certain ketone derivatives which have been synthesized. Two series of compounds, (A) and (B), were prepared to examine the relationship …
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Μελέτη των θέσεων δέσμευσης του L-γλουταμικού οξέος σε φυσιολογική και ατροφική ανθρώπινη παρεγκεφαλίδα: Συμβολή στη μελέτη της ελαιογεφυρο-παρεγκεφαλιδικής ατροφίας
The binding kinetics, pharmacological properties, ontogeny and localization of Cl⁻ dependent and/ CI⁻independent L-glutamate binding sites were studied in membrane preparations and sections of human cerebellum. Furthermore L-glutamate binding have been solubilized from the same membrane …
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Flexion and Extension : Studies Employing Muscles of the Shank in Amphibians
… have been used to compare physiological and pharmacological properties of flexor and extensor and to demonstrate various patterns of convulsion and their modification by depressants. Contractures have been investigated in the isolated organ bath. Depolarizing agents have been used to compare …
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Synthesis and biological evaluation of functionalized benzoxaboroles as potential antimicrobial agents
… to their unique electronic and physicochemical properties. B-hydroxy-1,2-oxaborolanes (benzoboroxoles) are a class of cyclic boronic acid derivatives and are highly important organic synthons because of their structural stability and their ability to undergo important C-C bond forming reactions …
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Synthesis and biological evaluation of antiparasitic Cysteine protease inhibitors based on the Isatin Scaffold
… (indole-2, 3-dione) possessing a wide range of pharmacological properties was used as a scaffold to which different moeities were appended. Potential inhibitors of parasitic cysteine proteases and three strains of P. falciparum were identified from synthesized libraries of compounds. Various …
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Synthesis and evaluation of benzoyl containing compounds as potential anti-cancer agents
… of the human body and operate effectively in its pharmacological properties. The research conducted in this investigation looks at a naturally occurring compound, Dibenzoyl methane (DBM), its derivatives, and a few additional synthesised compounds with similar chemical properties and their unique …
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Synthesis of α, β-Substituted Alkenylphosphonates from α-Phosphonovinyl Triflates: I) Palladium Catalyzed Suzuki-Miyaura Cross-coupling with Aryl Boronic Acids II) Palladium Catalyzed Reduction
… they have interesting chemical, biological and pharmacological properties. Vinylphosphonates are used in synthesis, polymer applications, and have demonstrated potential as anticancer and antimicrobial agents.</p> <p>Vinyl triflates are useful in organic synthesis and are referred to as …
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Design and synthesis of new potential anticancer agents and high-selective A2B antagonists
… compounds requires a wider analysis of their pharmacological properties. Also in this case, several compounds were synthesized. Some of them were tested in a radioligand binding assay to evaluate the affinity and selectivity toward A2BR subtype, further confirming the high potential of these …
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2,3-Dihalofenoles: sustratos de partida versátiles para la síntesis de heterociclos funcionalizados regioselectivamente
… a wide variety of compounds with biological or pharmacological properties. In this field, we have developed efficient routes to the synthesis of regioselectively functionalized indoles, benzo[b]furans and benzo[b]thiophenes. The directed ortho-metalation strategy in conjunction with …
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Neuronaalisten kolinergisten nikotiinireseptorien positiivinen ja negatiivinen allosteerinen modulaatio
… multiple different nAChR subtypes with different pharmacological properties. nAChRs participate extensively in physiological functions and pathophysiological conditions. nAChRs mediate the effects of endogenous agonist, acetylcholine, as well as commonly used substance of abuse, nicotine. …
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The Discovery and Development of Thienopyrimidines as Inhibitors of Helicobacter pylori
… model, suggesting further optimization of the pharmacological properties is required for this series. A scaffold hopping exercise was performed to discover novel scaffolds with improved ADME properties. The pyrrolopyrimidine 56 emerged with good anti-H. pylori activity, an improved solubility …
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