Synthesis And Evaluation Of A Novel Carbohydrate Template And Analogs Thereof For Potential Cns-Active Drugs, 2017 Seton Hall University
Synthesis And Evaluation Of A Novel Carbohydrate Template And Analogs Thereof For Potential Cns-Active Drugs, Emi Hanawa-Romero
Seton Hall University Dissertations and Theses (ETDs)
Central nervous system (CNS) disorders are becoming a major societal problem. Examples of well-known CNS disorders are: neurodegenerative disorders such as Parkinson's, Huntington's and Alzheimer’s diseases, epilepsy/seizures, addiction, bipolar disorder, catalepsy, meningitis, migraines, attention deficit/hyperactivity disorder (ADHD), and multiple sclerosis. CNS disorders can be caused by various factors and therefore can affect ages, genders and races of all.
The population of patients with CNS disorders is increasing and a significant percentage of patients have symptoms that are not controlled by existing treatments. In addition, since CNS disorders are chronic disorder, there is no cure and ...
Diversity Oriented Synthesis, Characterization And Anti-Cancer Activity Of Killer Peptide Nucleolipid Bioconjugates, Niki K. Rana
Seton Hall University Dissertations and Theses (ETDs)
The killer peptide sequence D-(KLAKLAK)2 has been originally designed and developed as an antibacterial agent. Despite having excellent cytotoxicity towards bacteria, this sequence maintains low cell cytotoxity in malignant mammalian cell types such as cancer. The chemical basis for its selectivity has been attributed to its poly(cationic) amphiphilic nature, which facilitates cell permeability across the negatively charged bacterial membrane, but with limited permeability across the zwitterionic membrane of mammalian cells. The positively charged D-(KLAKLAK)2 sequence has been found to accumulate on the surface of the mitochondria causing dissipation of the negatively charged mitochondrial membrane potential ...
Substituent Strength Vs Reactivity: A Study Of 1,3,4-Oxadiazoles And Electron Donating Groups, 2017 Otterbein University
Substituent Strength Vs Reactivity: A Study Of 1,3,4-Oxadiazoles And Electron Donating Groups, Katlynn Merringer
Honors Thesis Projects
This investigation focused on determining if there was a relationship between electron donating group substituent strength and resulting percent yield values of the 1,3,4-oxadiazole product. The data obtained from this investigation aimed to help chemists better understand the reactivity of the 1,3,4-oxadiazole because of its importance in the realm of drug design and development. In order to accomplish this, electron donating groups with varying pKa values were placed on the 1,3,4-oxadiazole and the resulting percent yields were analyzed for possible trends. The substituents used represented both resonance donating and inductively donating groups and were ...
The Role Of Nicotine, A7 Nicotinic Acetylcholine Receptors And Extracellular Matrix Remodeling In Pulmonary Fibrosis., 2016 University of Louisville
The Role Of Nicotine, A7 Nicotinic Acetylcholine Receptors And Extracellular Matrix Remodeling In Pulmonary Fibrosis., Glenn Ward Vicary
Electronic Theses and Dissertations
The median survival for idiopathic pulmonary fibrosis (IPF) patients from diagnosis is a dismal 3 years. This condition is characterized by pulmonary fibroproliferation and excess production and disordered deposition of extracellular matrix (ECM) proteins resulting in obliteration of the original tissue architecture, loss of lung function and eventual death due to respiratory failure. The main hindrance to the development of effective treatments against pulmonary fibrosis is the late detection of its progression and is often of unknown cause. Tobacco smoke represents the most important environmental factor linked to the development of pulmonary fibrosis, with over 60% of IPF patients current ...
Partial Amino Acid Sequence Of Lipid Transfer Protein From Fennel (Foeniculum Vulgare) Seeds, 2016 Chapman University
Partial Amino Acid Sequence Of Lipid Transfer Protein From Fennel (Foeniculum Vulgare) Seeds, Hasan Al-Shiyab, Caroline Aziz
Student Research Day Abstracts and Posters
Fennel (Foeniculum vulgare) is a biennial Egyptian medicinal plant with an aromatic odor that belongs to the family Apiaceae (Umbelliferae). Fennel seeds are commonly used in traditional medicine, as they are known to have anti-inflammatory, anti-fungal and anti-cancerous activities. The major constituents of the fennel plant are sugars, minerals, essential fatty acids, proteins and fibers. Although, there are numerous studies on the medicinal properties of essential oils of the fennel seeds, but there is limited data reported on the proteins and peptides. The aims of this project are to fully characterize the primary structure of proteins and to determine their ...
Assembly Of Nucleic Acid-Based Nanoparticles By Gas-Liquid Segmented Flow Microfluidics, 2016 Purdue University
Assembly Of Nucleic Acid-Based Nanoparticles By Gas-Liquid Segmented Flow Microfluidics, Matthew L. Capek, Ross Verheul, David H. Thompson
The Summer Undergraduate Research Fellowship (SURF) Symposium
The development of novel and efficient mixing methods is important for optimizing the efficiency of many biological and chemical processes. Tuning the physical and performance properties of nucleic acid-based nanoparticles is one such example known to be strongly affected by mixing efficiency. The characteristics of DNA nanoparticles (such as size, polydispersity, ζ-potential, and gel shift) are important to ensure their therapeutic potency, and new methods to optimize these characteristics are of significant importance to achieve the highest efficacy. In the present study, a simple segmented flow microfluidics system has been developed to augment mixing of pDNA/bPEI nanoparticles. This DNA ...
Countercurrent Chromatography Fractions Of Plant Extracts With Anti-Tuberculosis Activity, 2016 Olivet Nazarene University
Countercurrent Chromatography Fractions Of Plant Extracts With Anti-Tuberculosis Activity, Douglas Armstrong, Nathan C. Krause, Drew Frey, J. Brent Friesen, Baojie Wan, Jordan Gunn, Scott Franzblau
Faculty Scholarship – Chemistry
Samples of numerous plant species were received from the southwestern part of the USA, from Richard Spjut, and plant samples were collected here in Illinois. All were extracted with typical solvents, giving crude residues, some of which were subjected to chromatographic methods. Some of the crude residues and some of the fractions were tested for anti-tuberculosis activity and/or antibacterial activity.
In a general way, bioactive natural products are dealt with very well by Liang & Fang. More specifically, the southwestern part of the United States has a large variety of indigenous plants many of which have not been investigated for ...
The Effect Of Parathion On Red Blood Cell Acetylcholinesterase In The Wistar Rat, 2016 Sapporo Medical University
The Effect Of Parathion On Red Blood Cell Acetylcholinesterase In The Wistar Rat, Naofumi Bunya, Keigo Sawamoto, Hanif Benoit, Steven B. Bird
Open Access Articles
Organophosphorus (OP) pesticide poisoning is a significant problem worldwide. Research into new antidotes for these acetylcholinesterase inhibitors, and even optimal doses for current therapies, is hindered by a lack of standardized animal models. In this study, we sought to characterize the effects of the OP pesticide parathion on acetylcholinesterase in a Wistar rat model that included comprehensive medical care. Methods. Male Wistar rats were intubated and mechanically ventilated and then poisoned with between 20 mg/kg and 60 mg/kg of intravenous parathion. Upon developing signs of poisoning, the rats were treated with standard critical care, including atropine, pralidoxime chloride ...
Pioneering A Novel Class Of Tetrahydroimidazopyridines With Anti-Proliferative Property Study Against Prostate Cancer, 2016 Clark Atlanta University
Pioneering A Novel Class Of Tetrahydroimidazopyridines With Anti-Proliferative Property Study Against Prostate Cancer, Napoleon D'Cunha
Electronic Theses & Dissertations Collection for Atlanta University & Clark Atlanta University
The synthesis of tetrahydroimidazo[1,5-a]pyridine (rIMP) through the transfer hydrogenation of imidazo[1,5-a]pyridine (IMP) was successfully developed. The simple two-step procedure is the most viable and efficient method that results in a unique conjugated system with pyridine at the 1-position and functionalized phenyl group at the 3-position.
In the synthesis of imidazo[1,5-a]pyridine, the reaction between di-2-pyridil ketone, substituted benzaldehyde and ammonium acetate in acetic acid under N2 was highly successful, resulting in yields ranging from 35-95%. Highest yields were obtained for compounds that had electron withdrawing group on them.
The transfer hydrogenation ...
Characterization And Target Identification Of Ak301: A Novel Mitotic Arrest Agent, 2016 University of Connecticut
Characterization And Target Identification Of Ak301: A Novel Mitotic Arrest Agent, Michael J. Bond, Avijeet S. Chopra, Marina Bleiler, Michelle Yeagley, Eric Scocchera
University Scholar Projects
The Giardina Laboratory has recently identified AK301 as a novel mitotic arrest agent. This work aimed to characterize the arrest state induced by AK301 (EC50 ~ 150nM) and identify the cellar targets responsible for the arrest. It was found that AK301 arrest is readily reversible upon withdrawal of AK301. Cells that slip from mitosis after removal of AK301 are sensitized to apoptosis. This was found to be unique for AK301 when compared to other mitotic arrest agents like colchicine, vincristine, and BI2536. Arrested cells were found to have increased ATM activity as well as an upregulation of p53 and several ...
Renewable Resources: The New “Fossil Fuel”, 2016 Dominican University of California
Renewable Resources: The New “Fossil Fuel”, Christopher Huynh, Crystal Vinuya, Gabriel Samaniego, Desiree Caceres, Yessica Moran
Scholarly & Creative Works Conference 2017
Creating ethanol from renewable resources that can be found around our school campus.
Nitrogen And Phosphorus Availability From Various Composted Wastes For Use In Irish Agriculture And Horticulture, 2016 Dublin Institute of Technology
Nitrogen And Phosphorus Availability From Various Composted Wastes For Use In Irish Agriculture And Horticulture, Alan Lee
Current environmental EU legislation promotes recycling and recovery from organic waste products. Compost has been identified as an alternative to inorganic fertilisers and animal slurries as a nutrient source for crop plants. This study aimed to investigate nitrogen (N) and phosphorus (P) availability from various composted waste through detailed characterisations, complemented by short term lab incubations and long term plant growth experiments. Twenty-five composts were selected and classified by their groups. The composts were characterised by multiple different analytical techniques. Two incubation studies were conducted. One investigating N and P mineralisation potential of the composts and the second on the ...
Effects Of Nox-1 Inhibition On Real-Time Blood Nitric Oxide And Hydrogen Peroxide In Acute Hyperglycemia, 2016 Philadelphia College of Osteopathic Medicine
Effects Of Nox-1 Inhibition On Real-Time Blood Nitric Oxide And Hydrogen Peroxide In Acute Hyperglycemia, Ashley Mawhinney
PCOM Biomedical Studies Student Scholarship
Hyperglycemia has been associated with vascular endothelial dysfunction in part by a reduction in nitric oxide (NO) production and increased oxidative stress (e.g., increased superoxide (SO) and hydrogen peroxide (H2O2). Endothelial-derived NO can be significantly reduced by increased SO/H2O2 in part by the activation of NADPH oxidase during hyperglycemia. Of the 7 NADPH oxidase isoforms, NADPH oxidase isoform 1 (NOX1) is mainly expressed in the vasculature and may play a major role in hyperglycemia induced oxidative stress and vascular endothelial dysfunction. This hypothesis was tested by measuring blood NO and H2O2 levels ...
Piperlongumine (Piplartine) And Analogues: Antiproliferative Microtubule-Destabilising Agents, 2016 Trinity College Dublin, Ireland
Piperlongumine (Piplartine) And Analogues: Antiproliferative Microtubule-Destabilising Agents, Mary J. Meegan, Seema M. Nathwani, Brendan Twamley, Daniela M. Zisterer, Niamh O'Boyle
Piperlongumine (piplartine, 1) is a small molecule alkaloid that is receiving intense interest due to its antiproliferative and anticancer activities. We investigated the effects of 1 on tubulin and microtubules. Using both an isolated tubulin assay, and a combination of sedimentation and Western blotting, we demonstrated that 1 is a tubulin-destabilising agent. This result was confirmed by immunofluorescence and confocal microscopy, which showed that microtubules in MCF-7 breast cancer cells were depolymerised when treated with 1. We synthesised a number of analogues of 1 to explore structure-activity relationships. Compound 13 had the best cytotoxic profile of this series, showing potent ...
Synthesis And Biochemical Evaluation Of 3-Phenoxy-1,4-Diarylazetidin-2-Ones As Tubulin-Targeting Antitumor Agents, 2016 Trinity College Dublin
Synthesis And Biochemical Evaluation Of 3-Phenoxy-1,4-Diarylazetidin-2-Ones As Tubulin-Targeting Antitumor Agents, Thomas F. Greene, Shu Wang, Lisa M. Greene, Seema M. Nathwani, Jade K. Pollock, Azizah M. Malebari, Thomas Mccabe, Brendan Twamley, Niamh O'Boyle, Daniela M. Zisterer, Mary J. Meegan
Structure-activity relationships for a series of 3-phenoxy-1,4-diarylazetidin-2-ones were investigated leading to the discovery of a number of potent antiproliferative compounds, including trans-4-(3-hydroxy-4-methoxyphenyl)-3-phenoxy-1-(3,4,5-trimethoxyphenyl)azetidin-2-one (78b) and trans-4-(3-amino-4-methoxyphenyl)-3-phenoxy-1-(3,4,5-trimethoxyphenyl)azetidin-2-one (90b). X-ray crystallography studies indicate the potential importance of the torsional angle between the 1-phenyl ‘A’ ring and 4-phenyl ‘B’ ring for potent antiproliferative activity, and that a trans configuration between the 3-phenoxy and 4-phenyl rings is generally optimal. These compounds displayed IC50 values of 38 nM and 19 nM respectively in MCF-7 breast cancer cells, inhibited the polymerization ...
The Synthesis Of 1,3-Difluoro-2-Methyl-4-Phenylbenzene From A One-Pot Reaction Of Difluorocarbene And 1-Phenyl-2-Methylcyclobutene, Ruth Felicitas Menger
Senior Honors Projects
Previous studies show that 1,2-disubstituted cyclobutenes can be used in reaction with difluorocarbene to produce 1,3-difluorobenzenes. A pathway to the synthesis of these types of compounds is of interest due to their presence in fluoroquinolone antibacterials, resins, and insecticides. The synthesis is unique because the fluorine atoms from the difluorocarbene are not adjacent to each other when the ring expands to a benzene ring. This study focuses on the reaction of difluorocarbene with 1-phenyl-2-methylcyclobutene, which was synthesized in one-pot in 4 steps starting from 1-phenyl-1-propyne and zirconocene dichloride.
Can A Metallated Cyclen Species Be Used To Prepare New Odorants?, 2016 Virginia Commonwealth University
Can A Metallated Cyclen Species Be Used To Prepare New Odorants?, Jalynn Taylor-Farmer
Undergraduate Research Posters
Scientists in the fragrance industry are constantly searching for new odors to create as well as new, more efficient processes to create them. Scientists mainly look for new ways to synthesize fragrances that will reduce the impact on the environment, produce them at lower costs, produce higher yields, and sometimes to produce a more potent odor . In this research, we investigated the use of metallic macrocycles and/or metal-dioxygen chemistry to prepare new fragrances.
Cyclen (1,4,7,10-tetraazacyclododecane) has significant uses in many pharmaceutical and medicinal research developments such as advances in targeted cancer and Alzheimer’s agents ...
A Rare Case Report Of Probable Indigotindisulfonate Sodium-Induced Cardiac Arrest, 2016 Touro College of Pharmacy
A Rare Case Report Of Probable Indigotindisulfonate Sodium-Induced Cardiac Arrest, Andrew P. Smith, Catherine A. Millares-Sipin, Henry Cohen, William Lois
Touro College of Pharmacy (New York) Publications and Research
Background: Indigotindisulfonate (Indigo Carmine, American Regent, Shirely, NY) is a blue dye that is commonly used for localizing ureteral orifices during surgery. In general, it is safe and biologically inactive, with the package insert citing only rare idiosyncratic reactions and mild pressor effects in some patients. We report a case of a severe life-threatening anaphylactoid reaction due to indigotindisulfonate following intravenous administration.
Case Report: We describe a case of a 42-year-old female admitted for a total abdominal hysterectomy. Upon arrival to the operating room, her heart rate (HR) was 80/min, blood pressure (BP) was 135/75 mm Hg, and ...
Testing Novel Phenolic Fluorophores As Palladium Sensors At Different Concentrations, 2016 Wabash College
Testing Novel Phenolic Fluorophores As Palladium Sensors At Different Concentrations, Max Gallivan, Christopher Shrack Omsi, Laura Wysocki Ph.D.
MU-COM Research Day
Palladium is often used in the synthesis of Active Pharmaceutical Ingredients (APIs), although it is toxic to ingest. As it is difficult to remove, it is imperative to develop optimal palladium sensors that can be utilized in quality control of pharmaceutical synthesis in order to ensure that all residual palladium catalyst is removed from APIs. The goal of this project is to study a novel series of phenolic fluorophores in order see which, if any, are capable of functioning as palladium sensors. Through a Tsuji-Trost substitution reaction, palladium functions as a catalyst that facilitates the removal of the allyl group ...
Anti-Tb And Antibacterial Activities Of Natural Products Extracts, 2015 Olivet Nazarene University
Anti-Tb And Antibacterial Activities Of Natural Products Extracts, Douglas Armstrong, Nathan Krause, Drew Frey
Faculty Scholarship – Chemistry
Samples of numerous plant species were received from the southwestern part of the USA from Richard Spjut, and plant samples were collected here in Illinois. All were extracted with typical solvents, giving crude residues, some of which were subjected to counter-current or flash chromatographic methods. Some of the crude extracts and chromatographic fractions had anti-tuberculosis and/or antibacterial activity.
In a general way, bioactive natural products are dealt with very well by Liang & Fang, 2006. More specifically, the southwestern part of the United States has a large variety of indigenous plants, many of which have not been investigated for their ...