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Articles 1 - 26 of 26

Full-Text Articles in Organic Chemistry

Developing A Risk Assessment Protocol To Quantify Distribution And Uptake Of Persistent Organic Pollutants In Glacial Outflows, Kimberley Rain Miner May 2018

Developing A Risk Assessment Protocol To Quantify Distribution And Uptake Of Persistent Organic Pollutants In Glacial Outflows, Kimberley Rain Miner

Electronic Theses and Dissertations

Pollutants released by industrialized nations between 1960 and 2004 have been transported northward through atmospheric processes and deposited into glaciated alpine ecosystems. Many of these chemicals retain their original structure and are absorbed into the biota thousands of miles away from where they were originally utilized. With a warming climate increasing the melt of alpine glaciers, these glaciers may be introducing growing amounts of toxins into the watershed. While studies have demonstrated the existence of resident pollutants within glaciated ecosystems, no one has developed a risk assessment to identify sources and quantity of risk posed by these compounds when released ...


Chemical Investigation Of Antarctic Marine Organisms & Their Role In Modern Drug Discovery, Jacqueline Lee Fries Feb 2016

Chemical Investigation Of Antarctic Marine Organisms & Their Role In Modern Drug Discovery, Jacqueline Lee Fries

Graduate Theses and Dissertations

The chemicals produced by biological systems, whether proteins, peptides, or terpenes, will always provide an intriguing topic for researchers. Invisibly controlling every aspect of nature, these molecules are responsible for life, evolution, and death. Specifically, here is described the secondary metabolites produced by Antarctic marine organisms as well as others, and how they are used to defend or attract other animals while potentially providing health benefits to mankind. This is done through collection, extraction, and separation of individual specimens. The respective mixtures of compounds after isolation are then analyzed via spectroscopic methods such as nuclear magnetic resonance spectroscopy, mass spectrometry ...


Property-Guided Synthesis Of Tricyclic Indolines To Confront Antibiotic Resistance In Methicillin Resistant Staphylococcus Aureus, Patrick Michael Barbour Jan 2016

Property-Guided Synthesis Of Tricyclic Indolines To Confront Antibiotic Resistance In Methicillin Resistant Staphylococcus Aureus, Patrick Michael Barbour

Chemistry & Biochemistry Graduate Theses & Dissertations (1986-2018)

Antibiotics are essential to modern medicine. They have enabled surgery to become routine and allowed for the development of advanced treatments for cancer and burn patients. However, a reservoir of genes that confer resistance and aid in host colonization is distributed across the microbial world and decreases the ability of modern medicine to control infection. We have not been able to sustainably counteract this with new drugs and resistance has been observed for all antibiotics that have been employed in the clinic. New classes of antibiotics are needed, but we also need to explore ways to restore the efficacy of ...


Chemoenzymatic Studies To Enhance The Chemical Space Of Natural Products, Jhong-Min Chen Jan 2015

Chemoenzymatic Studies To Enhance The Chemical Space Of Natural Products, Jhong-Min Chen

Theses and Dissertations--Pharmacy

Natural products provide some of the most potent anticancer agents and offer a template for new drug design or improvement with the advantage of an enormous chemical space. The overall goal of this thesis research is to enhance the chemical space of two natural products in order to generate novel drugs with better in vivo bioactivities than the original natural products.

Polycarcin V (PV) is a gilvocarcin-type antitumor agent with similar structure and comparable bioactivity with the principle compound of this group, gilvocarcin V (GV). Modest modifications of the polyketide-derived tetracyclic core of GV had been accomplished, but the most ...


Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego F. Amado Torres May 2014

Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego F. Amado Torres

Diego Amado Torres

Proteins have the capacity to bind specific sets of compounds known as ligands, these are small molecules with a recurrent theme in their molecular design that is a characteristic exploited here to (i) identify particular affinities of small molecules for proteins with the aim of using them as ligands, inhibitors, or targeting moieties in more complex systems by means of a methodology that screens small molecules based on protein affinity; (ii) decorate a self-assembling supramolecular system at different positions, making it responsive to a complementary protein with the aim of exploring differences in disassembly and sensitivity of the release of ...


Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres Jan 2014

Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres

Doctoral Dissertations

Proteins have the capacity to bind specific sets of compounds known as ligands, these are small molecules with a recurrent theme in their molecular design that is a characteristic exploited here to (i) identify particular affinities of small molecules for proteins with the aim of using them as ligands, inhibitors, or targeting moieties in more complex systems by means of a methodology that screens small molecules based on protein affinity; (ii) decorate a self-assembling supramolecular system at different positions, making it responsive to a complementary protein with the aim of exploring differences in disassembly and sensitivity of the release of ...


Cytochrome P450 Family 1 Inhibitors And Structure-Activity Relationships, Jiawang Liu, Jayalakshmi Sridhar, Maryam Foroozesh Nov 2013

Cytochrome P450 Family 1 Inhibitors And Structure-Activity Relationships, Jiawang Liu, Jayalakshmi Sridhar, Maryam Foroozesh

Faculty and Staff Publications

With the widespread use of O-alkoxyresorufin dealkylation assays since the 1990s, thousands of inhibitors of cytochrome P450 family 1 enzymes (P450s 1A1, 1A2, and 1B1) have been identified and studied. Generally, planar polycyclic molecules such as polycyclic aromatic hydrocarbons, stilbenoids, and flavonoids are considered to potentially be effective inhibitors of these enzymes, however, the details of the structure-activity relationships and selectivity of these inhibitors are still ambiguous. In this review, we thoroughly discuss the selectivity of many representative P450 family 1 inhibitors reported in the past 20 years through a meta-analysis.


Comparative Metabolism Of Phenanthro[3,4-B]Thiophene And Benzo[C]Phenanthrene, Jaquan M. Williams Aug 2013

Comparative Metabolism Of Phenanthro[3,4-B]Thiophene And Benzo[C]Phenanthrene, Jaquan M. Williams

Jaquan M Williams

ABSTRACT OF THESIS Comparative Metabolism of Phenanthro[3,4-b]Thiophene And Benzo[c]Phenanthrene Polycyclic aromatic hydrocarbons (PAHs) and their sulfur-heterocyclic analogs (thia-PAHs) are commonly occurring persistent environmental contaminants formed by incomplete combustion of organic matter. A number of thia-PAHs have shown significant mutagenic and carcinogenic activities. As noted with PAHs, these chemical contaminants also require metabolic activation in order to exhibit their mutagenic and carcinogenic effects. In the present study, a comparison of the metabolism of highly mutagenic phenanthro[3,4-b]thiophene (P[3,4-b]T) and its weakly mutagenic carbon analogue, benzo[c]phenanthrene (B[c]P), was ...


The Reaction Of Methionine With A Non-C2-Symmetrical Platinum (Ii) Diamine Compound, Nilesh Sahi May 2012

The Reaction Of Methionine With A Non-C2-Symmetrical Platinum (Ii) Diamine Compound, Nilesh Sahi

Honors College Capstone Experience/Thesis Projects

The research that we have conducted has allowed us to discover that the amino acids, methionine (Met) and N-acetyl methionine (N-AcMet), will react in a 1:1 and 1:2 molar ratio with platinum complexes containing bulky diamine ligands. Previous research has allowed us to gain a plethora of information on the experimentation and results of specific bulky diamine ligands such as N,N,N',N'-tetramethylethylenediamine and N,N-diethylethylenediamine. In the current study, we have investigated the bulky diamine ligand of N,N-dimethylethylenediamine, or Me2en. With our focus on the bulk of the Me2en ligand ...


Evaluation Of Corn Furan Fatty Acid Putative Endocrine Disruptors On Reproductive Performance In Adult Female Chickens, K. W. Wilhelms, George A. Kraus, J. D. Schroeder, J. W. Kim, S. A. Cutler, M. A. Rasmussen, L. L. Anderson, C. G. Scanes Oct 2006

Evaluation Of Corn Furan Fatty Acid Putative Endocrine Disruptors On Reproductive Performance In Adult Female Chickens, K. W. Wilhelms, George A. Kraus, J. D. Schroeder, J. W. Kim, S. A. Cutler, M. A. Rasmussen, L. L. Anderson, C. G. Scanes

Chemistry Publications

Based on evidence from rodent models, it was hypothesized that furan fatty acids found in corn would inhibit reproduction in the laying hen. An isomeric mixture of furan fatty acids [9, (12)-oxy-10,13-dihydroxystearic acid and 10, (13)-oxy-9,12-dihydroxystearic acid] was administered for a period of 3 wk via the diet (1 and 3 ppm) at levels greater than those in corn to 20-wk-old pullets. There were no overt indications of acute or chronic toxicity (no effects on mortality, feed intake, or average daily gain). Similarly, there was no dose-dependent effect on reproductive parameters [egg production, egg weight, shell ...


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 ...


Enantiomeric Chromatographic Separations And Ionic Liquids , Jie Ding Jan 2005

Enantiomeric Chromatographic Separations And Ionic Liquids , Jie Ding

Retrospective Theses and Dissertations

The chiral nature of compounds contributes to their bioactivity and their various pharmaceutical/industrial uses. As a result, the Food and Drug Administration (FDA) has implemented policies for analyzing the enantiomers of chiral compounds. Gas chromatography (GC) and liquid chromatography (LC) utilizing chiral stationary phases are the two most commonly used methods to achieve direct enantiomeric separations of chiral compounds. The first part of this dissertation includes a review of direct separation of enantiomers in gas and liquid chromatography, an example of the enantiomeric separation of various racemic sulfoxides and sulfinate esters on four derivatized cyclodextrin chiral stationary phases using ...


New Palladium-Catalyzed Approaches To Heterocycles And Carbocycles, Qinhua Huang Jan 2004

New Palladium-Catalyzed Approaches To Heterocycles And Carbocycles, Qinhua Huang

Retrospective Theses and Dissertations

The tert-butylimines of o-(1-alkynyl)benzaldehydes and analogous pyridinecarbaldehydes have been cyclized under very mild reaction conditions in the presence of I2, ICl, PhSeCl, PhSCl and p-O2NC6H4SCl to give the corresponding halogen-, selenium- and sulfur-containing disubstituted isoquinolines and naphthyridines, respectively. Monosubstituted isoquinolines and naphthyridines have been synthesized by the metal-catalyzed ring closure of these same iminoalkynes. This methodology accommodates a variety of iminoalkynes and affords the anticipated heterocycles in moderate to excellent yields.;The Pd(II)-catalyzed cyclization of 2-(1-alkynyl)arylaldimines in the presence of various alkenes provides an efficient way to synthesize a variety of 4-(1-alkenyl)-3-arylisoquinolines ...


Synthesis Of Polycyclic Natural Products , Tuan Hoang Nguyen Jan 2003

Synthesis Of Polycyclic Natural Products , Tuan Hoang Nguyen

Retrospective Theses and Dissertations

Highly oxidized polycyclic natural products are abundant in nature and have diverse biological activities. Hyperforin has been identified as the sole constituent responsible for the antidepressant characteristic of St. John's wort. An approach to an oxidized bicyclic phloroglucin core of hyperforin is described. Puupehenone, a sesquiterpene found in marine sponges, has recently emerged as a strong candidate to treat tuberculosis. The synthesis of the BCD rings of puupehenone containing a quinone methide moiety is described.


Media Coverage Of Epa's Draft Dioxin Reassessment Report, Sharon M. Friedman, Megan A. Fitzpatrick, Brenda P. Egolf Jun 1999

Media Coverage Of Epa's Draft Dioxin Reassessment Report, Sharon M. Friedman, Megan A. Fitzpatrick, Brenda P. Egolf

RISK: Health, Safety & Environment (1990-2002)

Using content analysis, the authors examine the utility of news media in democratic decision making.


New Methods For The Synthesis Of Natural Products , Alexey G. Melekhov Jan 1999

New Methods For The Synthesis Of Natural Products , Alexey G. Melekhov

Retrospective Theses and Dissertations

In this work we developed new approaches to three different classes of compounds. In the first chapter we employed PIFA as an oxidant to develop a direct route to pyrrolobenzodiazepines. We also developed a new way to generate acyl radicals by oxidative decarboxylation. The utility of this methodology was shown in the synthesis of 8-deoxy DC-81. In the second chapter we developed a five-step synthetic route to 1,4-phenanthrenequinones. We also used one of these phenanthrenequinones for the construction of an angularly-fused aromatic systems. In the third chapter we studied Lewis acid-mediated cyclizations of acyl quinones. We synthesized a precursor ...


Total Synthesis Of Angularly Fused Natural Products , Guohua Zhao Jan 1996

Total Synthesis Of Angularly Fused Natural Products , Guohua Zhao

Retrospective Theses and Dissertations

The synthesis of angularly fused quinone natural product G-2N has been achieved using a photoenolization reaction and a Diels-Alder reaction in the key carbon-carbon bond forming steps. This route is direct and flexible. It should be applicable to synthesis of other analogous natural products;The skeleton of colchicine has been achieved using a Diels-Alder reaction followed by an electrophilic addition to the A ring as key steps. Our synthetic approach is direct. It could provide an efficient entry to total synthesis of colchicine.


Synthesis Of Diterpene Alkaloids , Tiberiu Mircea Siclovan Jan 1996

Synthesis Of Diterpene Alkaloids , Tiberiu Mircea Siclovan

Retrospective Theses and Dissertations

Aconitine, atisine and garrya type diterpene alkaloids show remarkable biological activity and have a number of structural features in common. Due to their complex structure, there is a discrepancy between progress made lately in the identification, isolation and characterization of new members of this family, on one hand, and successful efforts towards their total synthesis, on the other;Our synthetic studies led us to develop a highly reproducible synthesis of adamantane-containing compounds via the corresponding bridgehead anions;Studies on the application of functionalized bridgehead radicals in natural product synthesis resulted in the development of a versatile, mild and highly tolerant ...


A Quantitative Structure-Activity Relationship (Qsar) Study Of Chlorinated Cyclodiene Insecticide Analogs , Jianbo Liu Jan 1995

A Quantitative Structure-Activity Relationship (Qsar) Study Of Chlorinated Cyclodiene Insecticide Analogs , Jianbo Liu

Retrospective Theses and Dissertations

Quantitative structure-activity relationships (QSAR) between the inhibitory effect of specific t-butylbicyclophosphorothionate (TBPS) binding to rat brain P2 membrane, a lipophilic parameter, and topological indices, were studied for 33 chlorinated alicyclic insecticides such as heptachlor, aldrin and their structural analogs. This study shows that lipophilicity plays an important role in the action of cyclodiene compounds. The epoxide or ketone structural congeners, and the non-epoxide, non-ketone cyclodiene analogs exhibit two different QSARs and may bind to different regions, respectively, at the common GABA receptor. The epoxide or ketone congeners may bind at a slightly more hydrophilic region, and a negatively correlated linear ...


Synthetic Approaches To Huperzine A , Danette René Vines Jan 1994

Synthetic Approaches To Huperzine A , Danette René Vines

Retrospective Theses and Dissertations

The natural product huperzine A has been found to possess activity as a nootropic agent. Because of its memory facilitating effects, huperzine A represents a promising drug for the treatment of neurodegenerative diseases, such as Alzheimer's disease. As life expectancy increases, identifying and synthesizing drugs which treat cognitive dysfunction becomes a primary health objective;This study was undertaken to synthesize huperzine A, and to offer a direct route to improved analogs of huperzine A. A bicyclic amino ketone for the synthesis of huperzine A was prepared in six steps. The conjugate addition of metallated alkylpyridines afforded a direct route ...


Synthesis, Structure Features And Application Of Pro-Azaphsphatranes As Catalysts And Strong Non-Ionic Bases In Organic Synthesis , Jiansheng Tang Jan 1994

Synthesis, Structure Features And Application Of Pro-Azaphsphatranes As Catalysts And Strong Non-Ionic Bases In Organic Synthesis , Jiansheng Tang

Retrospective Theses and Dissertations

This dissertation describes the development of pro-azaphosphatranes ZP(MeNCH[subscript]2CH[subscript]2)[subscript]3N as versatile useful materials in organic synthesis;Pro-imidophosphatranes MeN= P(MeNCH[subscript]2CH[subscript]2)[subscript]3N and PhN= P(MeNCH[subscript]2CH[subscript]2)[subscript]3N, their corresponding acyclic analogues MeN= P(NMe[subscript]2)[subscript]3 and PhN= P(NMe[subscript]2)[subscript]3, and their conjugate acids as well as the conjugate acid of the commercially available non-ionic base P[subscript]4-t-Bu (i.e. t-BuN=P (N=P(NMe[subscript]2)[subscript]3][subscript]3) have been synthesized. Equilibria measured by [superscript ...


Fluorine And Sulfur Quinoline Derivatives As Antimalarial Agents , Leo Loveland Tolman Jan 1945

Fluorine And Sulfur Quinoline Derivatives As Antimalarial Agents , Leo Loveland Tolman

Retrospective Theses and Dissertations

Some of the theoretical aspects of synthetic antimalarials have been discussed;Series of each of the following types of compounds bars been prepared for antimalarial testings: aromatic compounds with sulfur-containing basic side-chains, trifluoromethyl derivatives, arsine derivatives, miscellaneous quinoline compounds containing basic side-chains, and some 2,5-dimethyl-1-pyrryl derivatives;The results of the pharmacological tests, which were carried out under the auspices of the United States Government, are restricted. Accordingly, publication of such results must wait on future release.


Synthetic Dibenzofurans Structurally Related To Known Analgesics, Frederick Albert Yeoman Jan 1944

Synthetic Dibenzofurans Structurally Related To Known Analgesics, Frederick Albert Yeoman

Retrospective Theses and Dissertations

No abstract provided.


The Physiological Action Of Some Furan Compounds , Willard H. Kirkpatrick Jan 1935

The Physiological Action Of Some Furan Compounds , Willard H. Kirkpatrick

Retrospective Theses and Dissertations

A review of the substitution reactions of dibenzofuran as been made. Both mono- and disubstitution reactions have been considered. The orientation of the nitration product of 3-acetaminodibenzofuran has been confirmed; and the structure of the bromination product of the 3-acetamino derivative has been established;Several N-substituted 3-aminodibenzofurans have been prepared for physiological tests. It has been shown that the Skraup reaction on aminodibenzofurans produces two isomeric pyrido-derivatives. Other derivatives in which the amino group was attached to side chains of various types in dibenzofuran have been synthesized and tested;The pharmacological reports revealed that the dibenzofuran derivatives investigated in the ...


Some Correlations Between Hypnotic Action And Chemical Constitution , William Glen Bywater Jan 1934

Some Correlations Between Hypnotic Action And Chemical Constitution , William Glen Bywater

Retrospective Theses and Dissertations

A review of theories of narcosis has been made, and some correlations between constitution and activity have been presented for the aliphatic hypnotics;The close and important relationship of dibenzofuran and its derivatives to morphine has been discussed. The following derivatives to morphine has been discussed. The following derivatives to morphine has been discussed. The following derivatives of dibenzofuran haven been prepared for use in physiological tests: 2-, 3-, and 4-amino-, 2- and 3-hydroxy-dibenzofuran, and 2- and 3-dibenzofurancarboxylic acids;A necessary study of nuclear substitution in dibenzofuran has been made prior to the preparation of derivatives for physiological tests. It ...


The Physiological Action Of Cystinyl Peptides And Guanidine Derivatives , H. James Harwood Jan 1931

The Physiological Action Of Cystinyl Peptides And Guanidine Derivatives , H. James Harwood

Retrospective Theses and Dissertations

A number of peptides consisting of cystine in combination with other amino acids found in insulin were prepared in the hope of finding a grouping which would show the hypoglucemic action of insulin;The compounds prepared were: dicarbethoxytyrosylcystine diethylester, dicarbethoxycystinyltyrosine ethylester, dicarbethoxycystinyltyrosine, dicarbethoxycystinylhistidine methylester and dicarbethoxycystinylarginine;The physiological tests of these compounds have not been completed.