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Synthesis Of 123-Iodine Labeled Rofecoxib Analogues: Potential Nuclear Medicine Imaging Agents, Brandy U. Belue

Masters Theses

Single photon emission computed tomography (SPECT) is a medical imaging technique which provides three-dimensional images ofliving systems after introduction ofa radiolabeled pharmaceutical. Rofecoxib (4-[ 4-methylsulphonylphenyl]-3phenylfuran-2(SH)-one) is an inhibitor of the cycloxygenase-2 enzyme, an enzyme which has been found to promote cancer cell growth. The synthesis of a no-carrier-added iodine-123 labeled rofecoxib derivative is potentially of value for the detection of cancer utilizing SPECT.

Iodine-123 labeled -(3-Iodophenyl)-4-(methanesulfonylphenyl)-SH furan-2-one, 1, and 3-(4-Iodophenyl)-4-(methanesulfonylphenyl)-5H-furan-2-one, 2, were prepared from the respective potassium organotrifluoroborate salts. The trifluoroborates were prepared from a simple six step pathway.

Systems For Predicting Pitzer’S Ion-Interaction Model Parameters, Theresa Balderas Obias

Masters Theses

Pitzer's Ion-interaction Model had been widely used in predicting the non-ideal behavior of solution over a wide range of conditions for natural water systems. The model is successful only when there are sufficient parameters available. However, generating these needed parameters requires a great quantity of work and it would be advantageous to be able to predict the Pitzer's parameters for salt systems when there is no data available.

This research entailed the development of ionic radii dependent equations for Pitzer's binary ion-interaction parameters β_MX⁽⁰⁾, β_MX⁽¹⁾, β_MX⁽²⁾, and C^ϕ_MX . …

Cloning, Overexpression, Purification And Characterization On N-Terminal Metal Binding Domains 5 And 6 Of Wilsons Disease Protein, David Achila

Masters Theses

Wilsons disease is an autosomal recessive disorder of copper metabolism which results from mutations in the gene encoding for Wilson disease protein (WDP). The cytosolic N-terminus of WDP comprises six metal binding domains each containing a conserved metal binding motif, GMXCXXC. The contribution of these metal binding domains to copper homeostasis is poorly understood. We have cloned, expressed and purified residues 485 to 633 corresponding to N-terminal metal-binding domains 5 and 6 of WDP (WD5-6). Two of the 3 disease causing mutations in the N-terminal metal binding domains of WDP occur one in each of these domains and the two …

Design, Synthesis And Characterization Of Nanosensors For Nerve Gas Agents, Thushara Gunasinghe

Masters Theses

This research is focused on the design synthesis and characterization of nanosensors to detect the nerve gas agents such as sarin at very low concentration levels (parts per billion and lower) which is very important to combat terrorism. Nanosensors constructed by the bottom up approach could provide the low sensitivity levels and high selectivity required for nerve gas detection. The sensing mechanism exploits the inherent properties of nanomaterials and signal amplification by signal transduction. The components of a nanoparticle-fluorescent monomer-nanomolecule-receptor (NMNR) sensor have been designed, synthesized, and characterized successfully. Interaction of the components of NMNR sensor with a model nerve …

Structure-Activity Relationship Studies On Thioxolone Compounds As Inhibitors Of Human Carbonic Anhydrase Ii, Jared Nyabuto Orwenyo

Masters Theses

Carbonic anhydrase II (CA II) is a zinc metalloenzyme that catalyzes the reversible hydration of carbon dioxide. The role of this reaction in physiology has made it a target of many therapeutic approaches. Most CA II inhibitors currently known are sulfonamide-based and this is the only functional group incorporated into rationally designed CA II inhibitors. Thioxolone (6-hydroxy-1, 3-benzoxathiol-2-one), is a non-sulfonamide that has been found to have CA II inhibitory activity.

Thioxolone and its analogs were studied to evaluate the inhibition activity that can be achieved upon modification of the thioxolone molecule. IC₅₀ values and dissociation constants were determined …

Ionic Liquid As Catalysts In The Cycloaddition Of Co2 To Styrene Oxide In Supercritical And Subcritical States, Joy Mwalimu

Masters Theses

Supercritical fluids (SCFs) have fascinated researchers ever since the discovery of a critical temperature more than a century ago.¹ Initial studies focused mainly on the physical properties of supercritical phases.² However, their use as reaction media has sparked mainly during the last five to ten years.²

The coupling of CO₂ and Ionic Liquids (ILs) in the synthesis of cyclic carbonates comes from an increasing need for environmentally and toxicologically benign processes for the production of high-value compounds. In my research, CO₂ was utilized as both a replacement solvent and a C₁ feedstock in its …

Thermodynamic Contributions Of Various Metal-Nucleotide Complexes Binding To Yeast Phosphoglycerate Kinase, Randall Allen Holzberger

Masters Theses

The purpose of this study was to determine the thermodynamic parameters of various enzyme-substrate complexes of Yeast Phosphoglycerate Kinase by using Isothermal Titration Calorimetry (ITC). The addition of metal-nucleotide substrate to a PGK solution elicited an exothermic response ranging from 0.5 kilocalories to 2.8 kilocalories. Titrations of MgATP and MgADP into PGK yielding binary complexes generated a greater amount of heat than titrations of MgADP into PGA-PGK and MgAMP-PCP into PGA-PGK yielding ternary complexes. The entropic contribution of the ternary complex formations was significantly greater than binary complex formations. Although entropic and enthalpic contributions varied, the Gibbs free energy remained …

Studies Of Alkaline Phosphatase Inhibition By Metal Chelators Using Capillary Electrophoresis, Courtney A. Neel

Masters Theses

Alkaline phosphatase inhibition by metal chelators has been studied using capillary electrophoresis. The enzyme-inhibition assays were performed by electrophoretically mixing enzyme and inhibitor zones in a substrate filled capillary. Enzyme inhibition could be seen as a decrease in product formation as detected using laser-induced fluorescence. The enzyme-inhibition assays were adapted so they could be performed using a commercial CE system. Use of a commercial system is desirable for these assays due to ease of use and system features such as autosamplers and capillary and sample cooling. This technique could prove useful for pharmaceutical industries as a screening tool for new …

Synthetic And Structural Studies Of Novel 1, 10-Phenanthroline Derivatives, Eunjoo Kim

Masters Theses

Asymmetric catalysis can provide a general approach to the preparation of enantiomerically enriched compounds in organic synthesis. Very often these asymmetric catalysts consist of a chiral ligand-metal complex. Because of the growing demand to develop enantioselective reactions in organic chemistry one focus of this area of research is the design and characterization of new chiral ligands for asymmetric synthesis.

The focus of my research is in the design, synthesis, and characterization of novel 1, 10-phenanthroline derivatives that could be used as chiral ligands in enantioselective reactions. Central to these studies have been the effect of substituents on the B-ring of …

Copper Exchange Studies Between The First And Fourth N-Terminal Metal-Binding Domains Of Wilson Disease Atpase, Jennifer Bunce

Masters Theses

The human copper-transporting ATPase Wilson's disease protein was one of the first proteins shown to be actively involved in cellular copper homeostasis. The protein includes six N-terminal metal binding domains. The individual capabilities of the domains to bind and transfer copper are not yet fully understood. Each metal-binding domain is about 72 amino acid residues long and contains the conserved binding motif GMTCXXC, of which the cysteines are involved in the copper coordination. Studies have shown that the protein binds six copper atoms suggesting the potential involvement of each metal-binding domain. Separate functional roles for the latter domains have been …

Rhizopine Synthesis – Potential Mediators For Nitrogen Fixation In Legume Plants, Venkat Reddy Guduru

Masters Theses

This research project focused on novel and efficient synthetic approaches of inosamine derivatives (rhizopines). The preparation of specific rhizopines would help elucidate the microbial pathway of rhizopine catabolism and degradation, and determine the role of corresponding genes during nitrogen fixation. We have investigated regio - and stereoselective transformations of myo-inositol derivative 28 utilizing an organostannane as key intermediate towards rhizopine 1a. The synthesis involved several protection and deprotection strategies to control competing reactivities of six hydroxyl groups of myo-inositol. Rhizopine 1a was prepared efficiently as a single isomer in 8 steps and 13% yield by controlling reactions …

Effect Of Antioxidants On Cadmium Induced Oxidative Stress And Signal Transduction, Deepti Goel

Masters Theses

A study was done to establish if reactive oxygen species (ROS) participate in the signal transduction pathway through which cadmium induces gene transcription. Cadmium has become a concern in the health care community in the past few years as evidence suggests that cadmium can induce the development of tumors, influence cell signaling and cause damage to organs, tissue, cells and DNA. The mechanism by which cadmium exerts its action on cellular processes or induces toxicity is however unclear although there is evidence to suggest that ROS play a role. Our laboratory is interested in understanding the mechanisms of differentially regulated …

Nonaqueous Platination For Synthesis Of Platinated 7 Alpha-Substituted Estradiol, Sarah A. Mazzella

Masters Theses

No abstract provided.

The Application Of 31p And 1h Nmr Spectroscopy To The Study Of Freeze Tolerance And Freeze Avoidance In Biological Systems, Nicholas C. Wright

Masters Theses

No abstract provided.