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Medicinal-Pharmaceutical Chemistry Commons

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2006

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Articles 1 - 12 of 12

Full-Text Articles in Medicinal-Pharmaceutical Chemistry

The Synthesis Of Zinc Oxide By Direct And Indirect Methods, Grainne Duffy Jul 2006

The Synthesis Of Zinc Oxide By Direct And Indirect Methods, Grainne Duffy

Masters

The synthesis of zinc oxide through three routes was investigated; carboxylic acid chelation, polymer assisted synthesis in an alcoholic medium and slow thermolysis of precursor. In the case of carboxylic acid chelation, it was determined that the rate at which the precursor is formed has a significant effect on the quality of zinc oxide particles produced. Investigation of the effect of concentration, pH and species of chelating agent used on the purity and structure of product was undertaken. Examination of the composition and morphology of materials produced revealed the presence of single-crystalline spheres, the packing density and aggregation morphology of ...


Secondary N-Nitrosocarbamate Anions: Structure And Alkylation Reactions. A Dft Study, Vladimir Benin May 2006

Secondary N-Nitrosocarbamate Anions: Structure And Alkylation Reactions. A Dft Study, Vladimir Benin

Chemistry Faculty Publications

The current article reports theoretical studies (DFT: B3LYP/6-31+G(d)) on the structure and alkylation reactions of the anions of some secondary N-nitrosocarbamates, a class of ambident nucleophiles whose chemistry has been little explored. Several anions (1–4), with an increasing size of the carbamate alkyl (aryl) group were investigated, in an attempt to establish the influence of the size of that group on the thermal stability and regioselectivity of alkylation of the title anions. The conclusion is that thermal stability and the mode of reaction are affected significantly only in the presence of very large and branched ...


Preparation Of Silica-Coated Lanthanum-Strontium Manganite Particles With Designable Curie Point, For Application In Hyperthermia Treatments, Vuk Uskoković, Aljoša Košak, Miha Drofenik Mar 2006

Preparation Of Silica-Coated Lanthanum-Strontium Manganite Particles With Designable Curie Point, For Application In Hyperthermia Treatments, Vuk Uskoković, Aljoša Košak, Miha Drofenik

Pharmacy Faculty Articles and Research

Silica-coated lanthanum–strontium manganite particles with La0.76Sr0.24MnO3+δ stoichiometric formula, exhibiting Curie temperature at ∼40°C, were prepared by using a traditional solid-state method of synthesis of magnetic ceramic particles, followed by milling and a low-temperature coating procedure in an aqueous alcoholic alkali medium. The properties of the obtained material establish it as a potential candidate for self-regulated power-absorbing and temperature-controlling materials in hyperthermia treatments. Moreover, core-comprising LaSr–manganites with different stoichiometries, ranging from La0.5Sr0.5MnO3+δ to LaMnO3+δ, were synthesized, with magnetic and structural ...


Limited Proteolysis Of Human Histone Deacetylase 1, Nayana Kamath, Paulina Karwowska-Desaulniers, Mary Kay H. Pflum Jan 2006

Limited Proteolysis Of Human Histone Deacetylase 1, Nayana Kamath, Paulina Karwowska-Desaulniers, Mary Kay H. Pflum

Wayne State University Associated BioMed Central Scholarship

Abstract

Background

Histone deacetylase (HDAC) proteins are associated with cell proliferation, differentiation, apoptosis, and cancer. Specifically, HDAC1 is linked with cell growth, a hallmark of cancer formation. HDAC1 is a phosphoprotein and phosphorylation at S421 and S423 promotes HDAC1 enzymatic activity and protein association. While single and double point mutants of HDAC1 at S421 and S423 appear functionally similar, the evidence suggests that HDAC1 is phosphorylated simultaneously at both S421 and S423 in vivo. Additional experiments are necessary to probe the role of double phosphorylation of HDAC1 at S421 and S423.

Results

To characterize HDAC1 phosphorylation at S421 and S423 ...


Preparation, Characterization And Dft Studies Of Some New N-Nitrosocarbamates And N-Nitrosoureas, Ragavan Narayanan, Helene Hedian, Eric Shamo, Vladimir Benin Jan 2006

Preparation, Characterization And Dft Studies Of Some New N-Nitrosocarbamates And N-Nitrosoureas, Ragavan Narayanan, Helene Hedian, Eric Shamo, Vladimir Benin

Chemistry Faculty Publications

We are presenting the preparation, characterization and density functional theory (DFT) studies {B3LYP/6-31+G(d)) of several reiated classes of N-nitrosocarbamates and N-nitrosoureas. The iong-range goal is the design and preparation of compounds, which would undergo photochemical or hydrolytic decomposition, to yield stabilized cyclic cations that can serve as alkylating agents at various nucleophilic centers, including DNA bases.


Preparation Of Some Substituted Terephthalic Acids, Susanna Branion, Vladimir Benin Jan 2006

Preparation Of Some Substituted Terephthalic Acids, Susanna Branion, Vladimir Benin

Chemistry Faculty Publications

We report in detail the preparation of two substituted terephthalic acids: 2‐sulfomethylterephthalic acid (1) and 2‐phosphonoterephthalic acid (2). Efficient, short syntheses have been developed for both compounds. They are potentially useful monomers for construction of acid‐pendant polymer chains.


Conformation Of The Acrb Multidrug Efflux Pump In Mutants Of The Putative Proton Relay Pathway, Chih-Chia Su, Ming Li, Ruoyu Gu, Yumiko Takatsuka, Gerry Mcdermott, Hiroshi Nikaido, Edward Yu Jan 2006

Conformation Of The Acrb Multidrug Efflux Pump In Mutants Of The Putative Proton Relay Pathway, Chih-Chia Su, Ming Li, Ruoyu Gu, Yumiko Takatsuka, Gerry Mcdermott, Hiroshi Nikaido, Edward Yu

Physics and Astronomy Publications

We previously reported the X-ray structures of wild-type Escherichia coli AcrB, a proton motive force-dependent multidrug efflux pump, and its N109A mutant. These structures presumably reflect the resting state of AcrB, which can bind drugs. After ligand binding, a proton may bind to an acidic residue(s) in the transmembrane domain, i.e., Asp407 or Asp408, within the putative network of electrostatically interacting residues, which also include Lys940 and Thr978, and this may initiate a series of conformational changes that result in drug expulsion. Herein we report the X-ray structures of four AcrB mutants, the D407A, D408A, K940A, and T978A ...


Cloning, Expression, Purification, Crystallization And Preliminary X-Ray Diffraction Analysis Of The Regulator Acrr From Escherichia Coli, Ming Li, Xi Qiu, Chih-Chia Su, Feng Long, Ruoyu Gu, Gerry Mcdermott, Edward Yu Jan 2006

Cloning, Expression, Purification, Crystallization And Preliminary X-Ray Diffraction Analysis Of The Regulator Acrr From Escherichia Coli, Ming Li, Xi Qiu, Chih-Chia Su, Feng Long, Ruoyu Gu, Gerry Mcdermott, Edward Yu

Physics and Astronomy Publications

This paper describes the cloning, expression, purification and preliminary X-ray data analysis of the AcrR regulatory protein. The Escherichia coli AcrR is a member of the TetR family of transcriptional regulators. It regulates the expression of the AcrAB multidrug transporter. Recombinant AcrR with a 6×His tag at the C-terminus was expressed in E. coli and purified by metal-affinity chromatography. The protein was crystallized using hanging-drop vapor diffusion. X-ray diffraction data were collected from cryocooled crystals at a synchrotron light source. The best crystal diffracted to 2.5 Å. The space group was determined to be P32, with ...


Nmr Studies Of Lysozyme Surface Accessibility By Using Different Paramagnetic Relaxation Probes, Andrea Bernini, Ottavia Spiga, Vincenzo Venditti, Filippo Prischi, Luisa Bracci, Angela Pui-Ling Tong, Wing-Tak Wong, Neri Niccolai Jan 2006

Nmr Studies Of Lysozyme Surface Accessibility By Using Different Paramagnetic Relaxation Probes, Andrea Bernini, Ottavia Spiga, Vincenzo Venditti, Filippo Prischi, Luisa Bracci, Angela Pui-Ling Tong, Wing-Tak Wong, Neri Niccolai

Vincenzo Venditti

Paramagnetic probes, whose approach to proteins can be monitored by nuclear magnetic resonance (NMR) studies, have been found to be of primary relevance for investigating protein surfaces' accessibility. Here, a Gd(III) neutral complex which contains two metal ions, [Gd2(L7)(H2O)2], is suggested as a paramagnetic probe particularly suited for systematic NMR investigation of protein surface accessibility, due to an expected high relaxivity and to the lack of electric charge which could favor specific interactions. Hen egg white lysozyme has been used as a model system to verify the absence of preferential approaches of this paramagnetic probe to ...


Synthesis Of Natural Compounds In Echinacea , Jaehoon Bae Jan 2006

Synthesis Of Natural Compounds In Echinacea , Jaehoon Bae

Retrospective Theses and Dissertations

In this dissertation, we have investigated the direct and efficient synthetic route to biologically active natural products. Chapter 1 describes the synthesis of some of the natural compounds in Echinacea. Several main constituents of the plant Echinacea have been synthesized for the first time. We have developed a direct and flexible route to amides and ketones in Echinacea. The synthesized natural products have been used for standard samples for the biological studies. Chapter 2 describes the new tandem strategy to construct bicyclic systems by a Diels-Alder/ene reaction and its application for the synthesis of Isoligularone. During this tandem reaction ...


A Minimum-Impact Method For Measuring Corrosion Rate Of Steel-Hulled Shipwrecks In Seawater, Matthew A. Russell, David L. Conlin, Larry E. Murphy, Donald L. Johnson, Brent M. Wilson, James D. Carr Jan 2006

A Minimum-Impact Method For Measuring Corrosion Rate Of Steel-Hulled Shipwrecks In Seawater, Matthew A. Russell, David L. Conlin, Larry E. Murphy, Donald L. Johnson, Brent M. Wilson, James D. Carr

Faculty Publications -- Chemistry Department

Current research on USS Arizona is focused on a minimum-impact technique for calculating corrosion rate of the battleship’s steel hull by analysing physical and chemical properties of marine encrustation covering the exposed hull. An equation is derived that allows concretion thickness, density, and total iron content to be used to calculate corrosion rate of steel hull plate.


Stability Of Warfarin Solutions For Drug–Protein Binding Measurements: Spectroscopic And Chromatographic Studies, Annette C. Moser, Charles A. Kingsbury, David S. Hage Jan 2006

Stability Of Warfarin Solutions For Drug–Protein Binding Measurements: Spectroscopic And Chromatographic Studies, Annette C. Moser, Charles A. Kingsbury, David S. Hage

Faculty Publications -- Chemistry Department

Warfarin is commonly used in drug–protein binding studies as a displacement marker for Sudlow site I on the protein human serum albumin (HSA). This study examined the stability of aqueous warfarin solutions prepared for such experiments. This was investigated using NMR spectroscopy and affinity chromatography. It was found by 1H NMR that warfarin underwent a slow first-order conversion in aqueous solution. The rate of this reaction increased with temperature, giving rate constants at pH 7.4 of 0.0086 h−1 at 25 °C and 0.041 h−1 at 37 °C. It was concluded from further 1H and ...