Chemistry Commons^™

Design, Synthesis & Biological Activity Of Novel Protein Tyrosine Phosphatase (Ptp) Mimetics, Sridhar Reddy Kaulagari

USF Tampa Graduate Theses and Dissertations

Protein phosphorylation is a post translational modification of proteins in which a serine, a threonine or a tyrosine residue is phosphorylated by an enzyme, kinase. Phosphorylation of proteins is a reversible and very important regulatory mechanism that occurs in both prokaryotes and eukaryotes. Phosphorylation turns many protein enzymes on and off, preventing or causing many diseases such as diabetes, cancer and rheumatoid arthritis. The phosphorylation on tyrosine residues of proteins is essential for transmission of signals for cell growth, proliferation and differentiation. Protein tyrosine phosphatases (PTPs) in concert with protein tyrosine kinases (PTKs) regulate many signal transduction pathways by controlling …

The Design And Synthesis Of Functionalized Porphyrins And Their Applications In Group Transfer Reactions, Medicine, And Materials, Kimberly Bliss Fields

USF Tampa Graduate Theses and Dissertations

Porphyrins and their analogs are a class of chemically and biologically important compounds that have found a variety of applications in different fields such as catalysis, medicine, and materials. The physical, chemical, and biological dependence of the peripheral substituents of porphyrins on their properties has prompted great effort towards the synthesis of new porphyrins with different electronic, steric, and conformational environments. To this end, porphyrins have been prepared using a modular approach from bromo- and triflate synthons. These synthons underwent palladium-catalyzed cross-coupling with chiral amines, amides, alcohols, and boronic esters to create products that were tested for biological activity.

Metalloporphyrins …

Synthesis Of Functionalized Resorcin[4]Arene Via Click Chemistry, Ali Husain

USF Tampa Graduate Theses and Dissertations

Click chemistry is a very powerful chemical strategy that overcome carbon-carbon bond with carbon-heteroatom bond by joining small units with heteroatom links (C-X-C) using spring-loaded reactants. The Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition is a major example based on the click chemistry philosophy. This method was used for the last 10 years to join different functional groups, carbohydrates, aminoacids, polymers to calix[4]arene and resorcin[4]arene cavitands by a stable 1,2,3-triazole linkages.

Herein I describe our interest in this type of click chemistry reaction in the synthesis of dimeric capsules resorcin[4]arene via four 1,2,3-triazole linkages. Two different resorcin[4]arene derivatives were synthesized in which four …

Applications Of Molecular Dynamics Techniques And Spectroscopic Theories To Aqueous Interfaces, Anthony Green

USF Tampa Graduate Theses and Dissertations

The primary goal of spectroscopy is to obtain molecularly detailed information about the system under study. Sum frequency generation (SFG) vibrational spectroscopy is a nonlinear optical technique that is highly interface specific, and is therefore a powerful tool for understanding interfacial structure and dynamics. SFG is a second order, electronically nonresonant, polarization experiment and is consequently dipole forbidden in isotropic media such as a bulk liquid. Interfaces, however, serve to break the symmetry and produce a signal. Theoretical approximations to vibrational spectra of O-H stretching at aqueous interfaces are constructed using time correlation function (TCF) and instantaneous normal mode (INM) …

Design And Combinatorial Synthesis Approach Of Non-Peptidic Trimeric Small Molecules Mimicking I, I + 4(3), I + 7 Positions Of Alpha-Helices, Mingzhou Zhou

USF Tampa Graduate Theses and Dissertations

Protein-protein interactions are key to several biological processes that facilitate signal transduction and many other processes. These interactions are involved in pathways that are critical to many human diseases. Targeting specific protein-protein interactions is a challenging goal because protein-protein interactions are predominately through hydrophobic interactions. Antagonists of the protein-protein interactions need to be perfectly fit into the binding pockets to ensure the activity. The -helical domain of the proteins behaves as the recognition motifs for numerous protein-protein, and protein-nucleic acid interactions. Research has shown that pathways of many diseases contain protein-protein interactions involving -helical domains, e.g. neurological disorders, bacterial infections, …

Design, Combinatorial Synthesis, And Biological Evaluation Of Novel Α-Helical Mimetics Based On Functionalized Piperazines As Antagonists Of P53/Mdm2 Interactions, Melissa Elizabeth Topper

USF Tampa Graduate Theses and Dissertations

The p53 protein promotes tumor eradication upon activation, making it an attractive target in cancer therapies. A reported 50% of all human cancers display aberrant activation of the MDM2 oncoprotein, which directly promotes tumorgenesis by inactivating the transcriptional activity of wild type p53, and is commonly associated with drug, chemo, and radio therapy resistance. Previously reported crystallographic analysis of the p53/MDM2 complex infers that the p53 protein forms a 2.5 turn amphipathic alpha helix whose hydrophobic face interacts within a deep hydrophobic cleft in the NH2-terminal domain of the globular MDM2. This suggests that the synthesis of small molecular antagonists …

Structural Diversity In Crystal Chemistry: Rational Design Strategies Toward The Synthesis Of Functional Metal-Organic Materials, Amy J. Cairns

USF Tampa Graduate Theses and Dissertations

Metal-Organic Materials (MOMs) represent an important class of solid-state crystalline materials. Their countless attractive attributes make them uniquely suited to potentially resolve many present and future utilitarian societal challenges ranging from energy and the environment, all the way to include biology and medicine. Since the birth of coordination chemistry, the self-assembly of organic molecules with metal ions has produced a plethora of simple and complex architectures, many of which possess diverse pore and channel systems in a periodic array. In its infancy however this field was primarily fueled by burgeoning serendipitous discoveries, with no regard to a rational design approach …

Chemical Investigation Of The Antarctic Marine Invertebrates Synoicum Adareanum And Artemisina Plumosa, Jaime Heimbegner Noguez

USF Tampa Graduate Theses and Dissertations

Of the small percentage of organisms chemically investigated over the years as potential sources of natural products, much less is known about those from the marine realm. Despite the lack of attention they have received in comparison to terrestrial organisms, marine life have recently been found to represent a valuable source for novel bioactive compounds. Cold water marine habitats are home to a plethora of organisms that have the ability to produce secondary metabolites that exhibit a great deal of diversity in both their chemical structures and biological activities. The chemical investigation of these unique and relatively unstudied ecosystems is …

Metal-Organic Materials: From Design Principles To Practical Applications, Mohamed H. Alkordi

USF Tampa Graduate Theses and Dissertations

The works presented herein outline rational design approaches towards construction of solid state materials with great potentials to answer some of current demanding applications. Specifically, the materials targeted are metal−organic materials with desirable structural features and functional properties. Metal−organic materials are constructed from organic linker molecules and metal ions under relatively mild solvothermal reaction conditions that preserve the structural features of the relatively simple building blocks. Therefore, it is feasible to conceive a retrospective pathway of the reaction and thus deconstruct the desirable structures into simple, chemicallyrelevant, building blocks in an approach known as the molecular building block approach. Due …

Functionalization Of Resorcinarenes And Study Of Antimicrobial Activity, Kirankirti Muppalla

USF Tampa Graduate Theses and Dissertations

Cavitands are very important class of compounds in supramolecular chemistry. These molecules contain rigid enforced cavity,and have attracted considerable attention in supramolecular chemistry as building blocks for the construction of carcerands, hemicarcerands, and other host guests complexes. Nearly 40 years ago, Niederl and Vogel laid foundation for the study of such type of condensation reactions. In our laboratory we are involved in synthesis of resorcinarenes with readily available substrates such as resorcinol and aldehydes to form a cyclic tetramer.

Herein, I present detailed studies about the functionalization of the synthesized tetramers and their antimicrobial activity. Octahydroxy resorcinarenes were synthesized and …

Jonas Kamlet (1914-1960) Chemist/Entrepreneur, Dean F. Martin, Barbara B. Martin

Chemistry Faculty Publications

Jonas Kamlet, Ph.D., as a chemist, inventor, and a significant entrepreneur who founded Kamlet Laboratories in New York City that became the model of a successful consulting firm. Among his hundreds of patents and inventions were a tablet that could be used to measure glucose in urine, a treated strip that could detect pregnancy, a fodder for ruminants that used newsprint, and biuret (a self-condensation product of urea) that could be used as a non-protein component of fodder. Following his death in an airplane collision on December 16, 1960, his wife and collaborator (and later a resident of Florida) carried …

An Investigation Into The Antifungal Activities Of N-Thiolated Beta- Lactams Against Selected Candida Species, Marci Culbreath

USF Tampa Graduate Theses and Dissertations

β-lactam antibiotics have long been a reliable course of treatment for bacterial infections. However, with recent increases in resistance and rising populations of immunocompromised patients new β-lactams have been synthesized and tested. The Turos laboratory has recently discovered novel β-lactams that have a mode of action distinct from penicillin and other β-lactam antibiotics as cell lysis is not observed. In the current investigations, these compounds are shown to also have antifungal properties. The rising incidence and prevalence of invasive fungal infections has become an increasing concern. The most common fungal pathogens involved in these infections are species in the genus …

Chemo-Enzymatic Route To Synthesis Of Biodegradable Polymers And Glycolipid Analogs, Surbhi Bhatt

USF Tampa Graduate Theses and Dissertations

New catalytic synthetic methods in organic chemistry that satisfy increasingly stringent environmental constraints are in great demand by the pharmaceutical and chemical industries. Studies over last 15 years have revealed that activity of enzymes can be increased in organic solvents rather than their natural aqueous environment. Because of their ease of use, high selectivity and environment friendliness, enzymes are enjoying increasing popularity in today's synthesis world.

Chapter 1 describes chemo-enzymatic synthesis of various glycolipid analogs. A highly regioselective macrolactonization was achieved using lipase from Candida antarctica as a catalyst. It also describes evaluation of lipases from different source and their …

The Growth And Toxicity Of The Florida Red Tide Organism, Gymnodinium Breve, Marion Tilton Doig Iii

USF Tampa Graduate Theses and Dissertations

Mass mortalities of marine organisms in the Gulf of Mexico have been associated with blooms of the unarmored dinoflagellate, Gymnodinium breve. This investigation concerns the factors affecting the growth of G. breve and the properties of a toxin produced by the organism.

A modification of the Flask Test of the Provisional Algal Assay Procedure of the Joint Industry/Government Task Force on Eutrophication was used to determine the response of G. breve to various natural waters and enrichments. The growth-promoting potential of natural waters obtained from areas where outbreaks of G. breve frequently occur was greater than that of waters …