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Synthesis Of Hydroxybenzylidene-Indolinones, Schiff Bases And N-Substituted Analogs And Their Effects On Bacterial Physiology., Catherine Eliana Cabrera, Neetu Dayal, Moloud Aflaki, Herman Sintim 2017 Universidad de Los Andes - Colombia

Synthesis Of Hydroxybenzylidene-Indolinones, Schiff Bases And N-Substituted Analogs And Their Effects On Bacterial Physiology., Catherine Eliana Cabrera, Neetu Dayal, Moloud Aflaki, Herman Sintim

The Summer Undergraduate Research Fellowship (SURF) Symposium

c-di-AMP is a global stress response regulator involved in some processes of biofilm formation and antibiotic resistance. It has become a candidate target for the development of new antibacterial treatments. Previous studies have shown that hydroxybenzylidene-indolinones can act as c-di-AMP synthase inhibitors. They also act as antibacterial and anti-biofilm inhibitors and re-sensitize resistant bacteria to methicillin and vancomycin. In this project, potent analogs of these compounds, including Schiff bases and N-substituted compounds, have been synthetized. The objective of this work is to explore the effect of these modifications on their biological activity. Base-catalyzed condensation and acid-catalyzed reactions were performed in ...


Computational Drug Design: A Multitargeted Approach In Bladder Cancer, Travis C. Lantz, Joydeb Majumder, Gaurav Chopra 2017 Purdue University

Computational Drug Design: A Multitargeted Approach In Bladder Cancer, Travis C. Lantz, Joydeb Majumder, Gaurav Chopra

The Summer Undergraduate Research Fellowship (SURF) Symposium

Cancer is a complex, robust disease with multiple redundant disease pathways which lead to tumor development, growth, and eventually even death. Despite known redundancies, cancer therapeutics continue to be developed against a single protein target. Initial disease regression occurs followed by relapse in a drug resistant disease state. In response, combinational drug clinical trial targeting multiple pathways began, and have failed due to increased toxicity caused by adverse drug interactions. Development of a single drug that differentially targets multiple disease pathways will result in a more potent therapeutic while inducing minimal toxicity. This was done computationally through in-lab software packages ...


Magnetic Field-Induced Intramolecular Cyclization As A Trigger For Nanoparticle-Based Delivery Systems., Sara Katherine Biladeau 2017 University of Louisville

Magnetic Field-Induced Intramolecular Cyclization As A Trigger For Nanoparticle-Based Delivery Systems., Sara Katherine Biladeau

Electronic Theses and Dissertations

Magnetic nanoparticles (MNPs) are used in a variety of applications, including as agents for magnetic resonance imaging, generation of local hyperthermia, and as platforms for drug delivery. Iron-based MNPs are often coated with a shell, such as silica or gold, to increase biocompatibility for drug delivery applications. Many MNPs used for cancer therapy rely on either an internal trigger, such as a difference in pH, or an external trigger, such as light or an alternating magnetic field (AMF), to cause release of a payload, typically a chemotherapeutic drug. Internal triggers are appealing because drug release can be targeted to a ...


Cellular And Molecular Targets Of Menthol Actions, Murat Oz, Eslam El Nebrisi, Keun-Hang Susan Yang, Frank Christopher Howarth, Lina T. Al Kury 2017 UAE University

Cellular And Molecular Targets Of Menthol Actions, Murat Oz, Eslam El Nebrisi, Keun-Hang Susan Yang, Frank Christopher Howarth, Lina T. Al Kury

Mathematics, Physics, and Computer Science Faculty Articles and Research

Menthol belongs to monoterpene class of a structurally diverse group of phytochemicals found in plant-derived essential oils. Menthol is widely used in pharmaceuticals, confectionary, oral hygiene products, pesticides, cosmetics, and as a flavoring agent. In addition, menthol is known to have antioxidant, anti-inflammatory, and analgesic effects. Recently, there has been renewed awareness in comprehending the biological and pharmacological effects of menthol. TRP channels have been demonstrated to mediate the cooling actions ofmenthol. There has been new evidence demonstrating thatmenthol can significantly influence the functional characteristics of a number of different kinds of ligand and voltage-gated ion channels, indicating that at ...


Synthesis And Evaluation Of A Novel Carbohydrate Template And Analogs Thereof For Potential Cns-Active Drugs, Emi Hanawa-Romero 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 2017 Seton Hall University

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, Katlynn Merringer 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 ...


Microtransplantation Of Rat Brain Neurolemma Into Xenopus Laevis Oocytes To Study The Effect Of Environmental Toxicants On Endogenous Voltage-Sensitive Ion Channels, Edwin Murenzi 2017 University of Massachusetts Amherst

Microtransplantation Of Rat Brain Neurolemma Into Xenopus Laevis Oocytes To Study The Effect Of Environmental Toxicants On Endogenous Voltage-Sensitive Ion Channels, Edwin Murenzi

Masters Theses

Microtransplantation of mammalian neurolemma into Xenopus laevis oocytes has been used to study ion channels in terms of their structure and function in the central nervous system. Use of microtransplanted neurolemma is advantageous in that tissue can be obtained from various sources, ion channels and receptors are present in their native configuration and they can be used to evaluate numerous channelpathies caused by environmental toxicants. Here we show that Xenopus oocytes injected with fragments of rat brain neurolemma successfully express functional native ion channels that are assembled in their own plasma membrane. Using a high throughput two electrode voltage clamp ...


Partial Amino Acid Sequence Of Lipid Transfer Protein From Fennel (Foeniculum Vulgare) Seeds, Hasan Al-Shiyab, Caroline Aziz 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 ...


The Role Of Nicotine, A7 Nicotinic Acetylcholine Receptors And Extracellular Matrix Remodeling In Pulmonary Fibrosis., Glenn Ward Vicary 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 ...


Assembly Of Nucleic Acid-Based Nanoparticles By Gas-Liquid Segmented Flow Microfluidics, Matthew L. Capek, Ross VerHeul, David H. Thompson 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, Douglas Armstrong, Nathan C. Krause, Drew Frey, J. Brent Friesen, Baojie Wan, Jordan Gunn, Scott Franzblau 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, Naofumi Bunya, Keigo Sawamoto, Hanif Benoit, Steven B. Bird 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, Napoleon D'Cunha 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, Michael J. Bond, Avijeet S. Chopra, Marina Bleiler, Michelle Yeagley, Eric Scocchera 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”, Christopher Huynh, Crystal Vinuya, Gabriel Samaniego, Desiree Caceres, Yessica Moran 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 2018

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, Alan Lee 2016 Dublin Institute of Technology

Nitrogen And Phosphorus Availability From Various Composted Wastes For Use In Irish Agriculture And Horticulture, Alan Lee

Doctoral

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 ...


A Rare Case Report Of Probable Indigotindisulfonate Sodium-Induced Cardiac Arrest, Andrew P. Smith, Catherine A. Millares-Sipin, Henry Cohen, William Lois 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, Max Gallivan, Christopher Shrack OMSI, Laura Wysocki Ph.D. 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 ...


Can A Metallated Cyclen Species Be Used To Prepare New Odorants?, Jalynn Taylor-Farmer 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 [4]. 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 ...


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