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Articles 1 - 26 of 26
Full-Text Articles in Chemicals and Drugs
Design And Synthesis Of Novel Sultams As Non-Nucleoside Inhibitors Of Hiv Reverse Transcriptase, Brian Chadwick Lecroix
Design And Synthesis Of Novel Sultams As Non-Nucleoside Inhibitors Of Hiv Reverse Transcriptase, Brian Chadwick Lecroix
Doctoral Dissertations
The compound 2-methyl-3-phenyl-2,3-dihydro-1,2-benzisothiazole 1,1-dioxide (NSC 108406) was identified as an HIV-1 reverse transcriptase inhibitor by the National Cancer Institute. Using this lead, the Baker group has developed a series of analogues with various groups at the 3-position that show a spectrum of biological activities. In the end, the substituents used could not compare to the biological activity of the inhibitor efavirenz (Sustiva® [trademark]), and so it was decided to synthesize sultams with alkylethynyl substituents at the 3-position of the sultams in an attempt to mimic the activity of efavirenz.
Previous research analyzed the proposed novel sultams in the modeling …
Developing A Presumptive Test For Select Synthetic Cannabinoids, Carrie Snyder
Developing A Presumptive Test For Select Synthetic Cannabinoids, Carrie Snyder
Graduate Theses and Dissertations
Synthetic cannabinoids (SC's) began to gain popularity around the world in 2009. Since then, many of the compounds have been outlawed and methods developed to detect them and their metabolites using mass spectrometry. Our work investigated the possibility of developing a colorimetric presumptive test. The SC JWH-019 was synthesized and its ketone targeted as a possible reaction site. Many SC's contain ketones and thus a reaction at this site would be applicable to many of the compounds. Since JWH-019 is costly and time consuming to synthesize, much of the experimental work was done using benzophenone (BP). BP contains a diaryl …
Formulation Development Of A Polymer-Drug Matrix With A Controlled Release Profile For The Treatment Of Glaucoma, Eric W. Tsoi
Formulation Development Of A Polymer-Drug Matrix With A Controlled Release Profile For The Treatment Of Glaucoma, Eric W. Tsoi
Master's Theses
Glaucoma is the leading cause of blindness in the United States accounting for 9-12% of all cases of blindness. Currently, the front line treatment for glaucoma are prostaglandins that may have to be taken up to several times a day. Even with proper treatment, roughly 11% of the patients using the treatment are non-compliant and lose their vision. In this project, ForSight Laboratories has developed a pharmaceutical drug delivering implant with the capability of sustaining long-term release of a prostaglandin as a new way to treat the condition. This project reports the product development of a polymer drug matrix with …
Single Step Synthesis Of Antibiotic Kanamycin Embedded Gold Nanoparticles For Efficient Antibacterial Activity, Shravan Gavva
Single Step Synthesis Of Antibiotic Kanamycin Embedded Gold Nanoparticles For Efficient Antibacterial Activity, Shravan Gavva
Masters Theses & Specialist Projects
Nanotechnology has become the most advanced type of drug delivery system within the last decade. This advancement shifted the focus on small carriers to increase the efficiency of the drugs. Among these, gold nanoparticles (GNPs) were found to have profound biomedical applications. In current research, kanamycin embedded GNPs were prepared in a single step, single phase, and bio-friendly (green synthesis) procedure. The synthesized Kanamycin-GNPs (Kan-GNPs) were spherical in shape and had a size range of 15 ± 3 nm. The chosen kanamycin is an aminoglycosidic antibiotic that is isolated from Streptomyces kanamyceticus. These special antibiotic GNPs are further characterized using …
Ionic Conductivity In Non-Ionic Compounds, Usha Kranthi Avala
Ionic Conductivity In Non-Ionic Compounds, Usha Kranthi Avala
Masters Theses & Specialist Projects
The main objective of this work is to investigate the ionic conductivity of the drugs under certain conditions and also to compare the ionic conductivities of drugs determined by single surface sensors and parallel plate sensors. The ionic conductivity of various materials at their pre-melt and melt states are studied in order to further study a recently discovered phenomenon. Polar solids like Lidocaine, Ketoconazole, Procainamide and Nifedipine were examined in this study. Experimental studies show an increase in ionic conductivity in both pre-melt (20 -30 °C below melting temperature) and melt transition regions. Results of ionic conductivity of both parallel …
Developing Thyronamine Analog Pharmaceuticals Targeting Taar1 To Treat Methamphetamine Addiction, Troy Andrew Wahl
Developing Thyronamine Analog Pharmaceuticals Targeting Taar1 To Treat Methamphetamine Addiction, Troy Andrew Wahl
Dissertations and Theses
As a part of the overall program in the Grandy laboratory at Oregon Health & Science University (OHSU), studying the underlying chemical biology of methamphetamine (Meth) addiction, this dissertation reports on the development of six new thyronamine analogs which were synthesized and assayed against trace amine associated receptor 1 (TAAR1), giving preliminary results consistent with the analogs being inverse agonists. Due to highly variable TAAR1 expression levels in the assays, based on inter-assay response to control Meth stimulation as well as other possible factors, kinetic models were developed to qualitatively explain the assay results. The models set approximate limits on …
Warfarin Use And Outcomes In Patients With Advanced Chronic Systolic Heart Failure Without Atrial Fibrillation, Prior Thromboembolic Events, Or Prosthetic Valves, Marjan Mujib, Abu-Ahmed Rahman, Ravi Desai, Mustafa Ahmed, Margaret Feller, Inmaculada Aban, Tomas Love, Michel White, Prakash Deedwania, Wilbert Aronow, Gregg Fonarow, Ali Ahmed
Warfarin Use And Outcomes In Patients With Advanced Chronic Systolic Heart Failure Without Atrial Fibrillation, Prior Thromboembolic Events, Or Prosthetic Valves, Marjan Mujib, Abu-Ahmed Rahman, Ravi Desai, Mustafa Ahmed, Margaret Feller, Inmaculada Aban, Tomas Love, Michel White, Prakash Deedwania, Wilbert Aronow, Gregg Fonarow, Ali Ahmed
Ravi V Desai MD
No abstract provided.
Influence Of Co-Existing Atrial Fibrillation On The Efficacy Of Atorvastatin Treatment In Patients With Dilated Cardiomyopathy: A Pilot Study, Agata Bielecka-Dabrowa, Jan Goch, Jacek Rysz, Marek Maciejewski, Ravi Desai, Wilbert Aronow
Influence Of Co-Existing Atrial Fibrillation On The Efficacy Of Atorvastatin Treatment In Patients With Dilated Cardiomyopathy: A Pilot Study, Agata Bielecka-Dabrowa, Jan Goch, Jacek Rysz, Marek Maciejewski, Ravi Desai, Wilbert Aronow
Ravi V Desai MD
No abstract provided.
Relationship Between Left And Right Ventricular Ejection Fractions In Chronic Advanced Systolic Heart Failure: Insights From The Best Trial, Ravi Desai, Philippe Meyer, Mustafa Ahmed, Marjan Mujib, Chris Adamopoulos, Michel White, Inmaculada Aban, Ami Iskandrian, Ali Ahmed
Relationship Between Left And Right Ventricular Ejection Fractions In Chronic Advanced Systolic Heart Failure: Insights From The Best Trial, Ravi Desai, Philippe Meyer, Mustafa Ahmed, Marjan Mujib, Chris Adamopoulos, Michel White, Inmaculada Aban, Ami Iskandrian, Ali Ahmed
Ravi V Desai MD
No abstract provided.
Identification Of Cisplatin-Binding Proteins Using Agarose Conjugates Of Platinum Compounds, Takatoshi Karasawa, Martha Sibrian-Vazquez, Robert M. Strongin, Peter S. Steyger
Identification Of Cisplatin-Binding Proteins Using Agarose Conjugates Of Platinum Compounds, Takatoshi Karasawa, Martha Sibrian-Vazquez, Robert M. Strongin, Peter S. Steyger
Chemistry Faculty Publications and Presentations
Cisplatin is widely used as an antineoplastic drug, but its ototoxic and nephrotoxic side-effects, as well as the inherent or acquired resistance of some cancers to cisplatin, remain significant clinical problems. Cisplatin’s selectivity in killing rapidly proliferating cancer cells is largely dependent on covalent binding to DNA via cisplatin’s chloride sites that had been aquated. We hypothesized that cisplatin’s toxicity in slowly proliferating or terminally differentiated cells is primarily due to drug-protein interactions, instead of drug-DNA binding. To identify proteins that bind to cisplatin, we synthesized two different platinum-agarose conjugates, one with two amino groups and another with two chlorides …
Label-Free Detection Of Low Protein Concentration In Solution Using A Novel Colorimetric Assay, Molla R. Islam, Michael J. Serpe
Label-Free Detection Of Low Protein Concentration In Solution Using A Novel Colorimetric Assay, Molla R. Islam, Michael J. Serpe
Biology, Chemistry, and Environmental Sciences Faculty Articles and Research
Dual pH and temperature sensitive microgel-based etalons were fabricated by sandwiching a “monolithic” microgel layer between two semitransparent, Au layers. The devices exhibit visual color and multipeak reflectance spectra, both of which primarily depend on the distance between the Au surfaces mediated by the microgel diameter. We found that a polycationic polyelectrolyte can penetrate through the Au overlayer to interact with negatively charged microgel confined between Au overlayers. In this submission we report that biotinylated polycationic polymer can penetrate through the Au overlayer of a poly (N-isopropylacrylamide)-co-acrylic acid (pNIPAm-co-AAc) microgel-based etalon and cause the microgel layer to collapse. The collapse …
Effect Of Leaving Ligands Of Platinum(Ii) Diamine Complexes On Dna And Protein Residues, Ramya Kolli
Effect Of Leaving Ligands Of Platinum(Ii) Diamine Complexes On Dna And Protein Residues, Ramya Kolli
Masters Theses & Specialist Projects
Platinum compounds are widely used drugs in cancer treatments. Although DNA is the biological target, reaction of platinum compounds with proteins is also potentially significant. Our objective is to study the effects of leaving ligands on the relative reactivity between 5'-GMP (guanosine 5' phosphate), a key DNA target, and N-Acetyl - L-Methionine (N-AcMet), a key protein target. We have used NMR spectroscopy to monitor reactions with N-AcMet and 5'-GMP added to a platinum complex to see which products are formed preferentially. Previous research showed that both a non-bulky complex such as [Pt(en)(D2O)2]2+ [en=ethylenediamine], and a …
Comparison Of Methodologies For Synthesis Of 3-(Cyclopropylethynyl)Benzisothiazole 1,1-Dioxide, Rachel Lee Naramore
Comparison Of Methodologies For Synthesis Of 3-(Cyclopropylethynyl)Benzisothiazole 1,1-Dioxide, Rachel Lee Naramore
Chancellor’s Honors Program Projects
No abstract provided.
A Mathematical Model For Antibiotic Resistance In A Hospital Setting With A Varying Population, Edward H. Snyder
A Mathematical Model For Antibiotic Resistance In A Hospital Setting With A Varying Population, Edward H. Snyder
Electronic Theses and Dissertations
Antibiotic-resistant bacteria(ARB) is causing increased health risk and cost to society. Mathematical models have been developed to study the transmission of resistant bacteria and the efficacy of preventive measures to slow its spread within a hospital setting. The majority of these models have assumed a constant total hospital population with the admission and discharge rates being equal throughout the duration. But a typical hospital population varies from day to day and season to season. In this thesis, we apply variable admission and discharge daily rates to existing deterministic and stochastic models which examine the transmission of single and dual resistant …
Compliance With The Centers For Disease Control And Prevention Recommendations For The Diagnosis And Treatment Of Sexually Transmitted Diseases, Bryan Kane, Linda Degutis, Helen Sayward, Gail D'Onofrio
Compliance With The Centers For Disease Control And Prevention Recommendations For The Diagnosis And Treatment Of Sexually Transmitted Diseases, Bryan Kane, Linda Degutis, Helen Sayward, Gail D'Onofrio
Bryan G Kane MD
No abstract provided.
Development Of A Rapid Spme/Gc-Ms Method For The Detection And Quantification Of Synthetic Cathinones In Oral Fluid, David Correll
Development Of A Rapid Spme/Gc-Ms Method For The Detection And Quantification Of Synthetic Cathinones In Oral Fluid, David Correll
Senior Theses and Projects
The recent emergence and widespread abuse of new classes of compounds on the designer drug market as “legal” alternatives to scheduled drugs such as Ecstasy has prompted interest in the development of analytical methods for their detection and characterization. Synthetic cathinones, which are structurally similar to amphetamines, are commonly advertised as a “legal highs” or “herbal highs,” and are marketed under names such as “bath salts” and “plant food.” To avoid drug abuse legislation, a “not for human consumption” warning is typically printed on the label. Their ready availability on the Internet and in “head” shops, convenience stores, and even …
Dimethyl Sulfoxide (Dmso) Exacerbates Cisplatin-Induced Sensory Hair Cell Death In Zebrafish (Danio Rerio), Phillip M. Uribe, Melissa A. Mueller, Julia S. Gleichman, Matthew D. Kramer, Qi Wang, Martha Sibrian-Vazquez, Robert M. Strongin, Peter S. Steyger, Douglas A. Cotanche, Jonathan I. Matsui
Dimethyl Sulfoxide (Dmso) Exacerbates Cisplatin-Induced Sensory Hair Cell Death In Zebrafish (Danio Rerio), Phillip M. Uribe, Melissa A. Mueller, Julia S. Gleichman, Matthew D. Kramer, Qi Wang, Martha Sibrian-Vazquez, Robert M. Strongin, Peter S. Steyger, Douglas A. Cotanche, Jonathan I. Matsui
Chemistry Faculty Publications and Presentations
Inner ear sensory hair cells die following exposure to aminoglycoside antibiotics or chemotherapeutics like cisplatin, leading to permanent auditory and/or balance deficits in humans. Zebrafish (Danio rerio) are used to study drug-induced sensory hair cell death since their hair cells are similar in structure and function to those found in humans. We developed a cisplatin dose-response curve using a transgenic line of zebrafish that expresses membrane-targeted green fluorescent protein under the control of the Brn3c promoter/enhancer. Recently, several small molecule screens have been conducted using zebrafish to identify potential pharmacological agents that could be used to protect sensory hair cells …
Atrazine And Nitrate In Public Drinking Water Supplies And Non-Hodgkin Lymphoma In Nebraska, Usa, Martha G. Rhoades, Jane L. Meza, Cheryl L. Beseler, Patrick J. Shea, Andy Kahle, Julie M. Vose, Kent M. Eskridge, Roy F. Spalding
Atrazine And Nitrate In Public Drinking Water Supplies And Non-Hodgkin Lymphoma In Nebraska, Usa, Martha G. Rhoades, Jane L. Meza, Cheryl L. Beseler, Patrick J. Shea, Andy Kahle, Julie M. Vose, Kent M. Eskridge, Roy F. Spalding
School of Natural Resources: Faculty Publications
A secondary analysis of 1999–2002 Nebraska case-control data was conducted to assess the risk of non-Hodgkin lymphoma (NHL) associated with exposure to nitrate- and atrazine-contaminated drinking water. Water chemistry data were collected and weighted by well contribution and proximity of residence to water supply, followed by logistic regression to determine odds ratios (OR) and 95% confidence intervals (CI). We found no association between NHL risk and exposure to drinking water containing atrazine or nitrate alone. Risk associated with the interaction of nitrate and atrazine in drinking water was elevated (OR, 2.5; CI, 1.0–6.2). Risk of indolent B-cell lymphoma was higher …
Chlomid, Niki Smith
Chlomid, Niki Smith
Natural Sciences Student Research Presentations
This poster details the use of Clomid and provides a chemical analysis.
Lyrica, Shannon Hayward
Lyrica, Shannon Hayward
Natural Sciences Student Research Presentations
Illustrates the chemical components of Lyrica, a pain management medication.
Development Of Affinity Microcolumns For Drug–Protein Binding Studies In Personalized Medicine: Interactions Of Sulfonylurea Drugs With In Vivo Glycated Human Serum Albumin, Jeanethe Anguizola, K. S. Joseph, Omar S. Barnaby, Ryan Matsuda, Guadalupe Alvarado, William Clarke, Ronald Cerny, David S. Hage
Development Of Affinity Microcolumns For Drug–Protein Binding Studies In Personalized Medicine: Interactions Of Sulfonylurea Drugs With In Vivo Glycated Human Serum Albumin, Jeanethe Anguizola, K. S. Joseph, Omar S. Barnaby, Ryan Matsuda, Guadalupe Alvarado, William Clarke, Ronald Cerny, David S. Hage
David Hage Publications
This report used high-performance affinity microcolumns to examine the changes in binding by sulfonylurea drugs to in vivo glycated HSA that had been isolated from individual patients with diabetes. An immunoextraction approach was developed to isolate HSA and glycated HSA from clinical samples, using only 20 μL of plasma or serum and 6–12 nmol of protein to prepare each affinity microcolumn. It was found that the affinity microcolumns could be used in either frontal analysis or zonal elution studies, which typically required only 4–8 min per run. The microcolumns had good stability and allowed data to be obtained for multiple …
Structural Basis For Enzyme I Inhibition By Α-Ketoglutarate, Vincenzo Venditti, Rodolfo Ghirlando, G. Marius Clore
Structural Basis For Enzyme I Inhibition By Α-Ketoglutarate, Vincenzo Venditti, Rodolfo Ghirlando, G. Marius Clore
Vincenzo Venditti
Creating new bacterial strains in which carbon and nitrogen metabolism are uncoupled is potentially very useful for optimizing yields of microbial produced chemicals from renewable carbon sources. However, the mechanisms that balance carbon and nitrogen consumption in bacteria are poorly understood. Recently, α-ketoglutarate (αKG), the carbon substrate for ammonia assimilation, has been observed to inhibit Escherichia coli enzyme I (EI), the first component of the bacterial phosphotransferase system (PTS), thereby providing a direct biochemical link between central carbon and nitrogen metabolism. Here we investigate the EI-αKG interaction by NMR and enzymatic assays. We show that αKG binds with a KD …
Structure, Dynamics And Biophysics Of The Cytoplasmic Protein–Protein Complexes Of The Bacterial Phosphoenolpyruvate: Sugar Phosphotransferase System, Vincenzo Venditti
Structure, Dynamics And Biophysics Of The Cytoplasmic Protein–Protein Complexes Of The Bacterial Phosphoenolpyruvate: Sugar Phosphotransferase System, Vincenzo Venditti
Vincenzo Venditti
The bacterial phosphotransferase system (PTS) couples phosphoryl transfer, via a series of bimolecular protein–protein interactions, to sugar transport across the membrane. The multitude of complexes in the PTS provides a paradigm for studying protein interactions, and for understanding how the same binding surface can specifically recognize a diverse array of targets. Fifteen years of work aimed at solving the solution structures of all soluble protein–protein complexes of the PTS has served as a test bed for developing NMR and integrated hybrid approaches to study larger complexes in solution and to probe transient, spectroscopically invisible states, including encounter complexes. We review …
Raman Micro Spectroscopy Study Of The Interaction Of Vincristine With A549 Cells Supported By Expression Analysis Of Bcl-2 Protein, Haq Nawaz, Amaya Garcia, Aidan Meade, Fiona Lyng, Hugh Byrne
Raman Micro Spectroscopy Study Of The Interaction Of Vincristine With A549 Cells Supported By Expression Analysis Of Bcl-2 Protein, Haq Nawaz, Amaya Garcia, Aidan Meade, Fiona Lyng, Hugh Byrne
Articles
Understanding the interaction of anticancer drugs with model cell lines is important to elucidate the mode of action of these drugs as well as to develop cost effective and rapid screening methods. Raman spectroscopy has been demonstrated to be a valuable technique for high throughput, noninvasive analysis. The interaction of vincristine with a human lung adenocarcinoma cell line (A549)was investigated using Raman micro spectroscopy. The results were correlated with parallel measurements from the MTT cytotoxicity assay, which yielded an IC50 value of 0.10 ± 0.03 μM. The Raman spectral data acquired from vincristine treated A549 cells was analysed to …
Revisiting The Fundamentals In The Design And Control Of Nanoparticulate Colloids In The Frame Of Soft Chemistry, Vuk Uskoković
Revisiting The Fundamentals In The Design And Control Of Nanoparticulate Colloids In The Frame Of Soft Chemistry, Vuk Uskoković
Pharmacy Faculty Articles and Research
This review presents thoughts on some of the fundamental features of conceptual models applied in the design of fine particles in the frames of colloid and soft chemistry. A special emphasis is placed on the limitations of these models, an acknowledgment of which is vital in improving their intricacy and effectiveness in predicting the outcomes of the corresponding experimental settings. Thermodynamics of self-assembly phenomena illustrated on the examples of protein assembly and micellization is analyzed in relation to the previously elaborated thesis that each self-assembly in reality presents a co-assembly, since it implies a mutual reorganization of the assembling system …
Turning Stealth Liposomes Into Cationic Liposomes For Anticancer Drug Delivery, Vijay Gyanani
Turning Stealth Liposomes Into Cationic Liposomes For Anticancer Drug Delivery, Vijay Gyanani
University of the Pacific Theses and Dissertations
Targeting the anticancer agents selectively to cancer cells is desirable to improve the efficacy and to reduce the side effects of anticancer therapy. Previously reported passive tumor targeting by PEGylated liposomes (stealth liposomes) have resulted in their higher tumor accumulation. However their interaction with cancer cells has been minimal due to the steric hindrance of the PEG coating. This dissertation reports two approaches to enhance the interaction of stealth liposomes with cancer cells. First, we designed a lipid-hydrazone-PEG conjugate that removes the PEG coating at acidic pH as in the tumor interstitium. However, such a conjugate was highly unstable on …