Open Access. Powered by Scholars. Published by Universities.®

Organic Chemicals Commons

Open Access. Powered by Scholars. Published by Universities.®

164 Full-Text Articles 331 Authors 42,770 Downloads 49 Institutions

All Articles in Organic Chemicals

Faceted Search

164 full-text articles. Page 1 of 7.

In Vitro And Ex-Vivo Evaluation Of Topical Formulations Designed To Minimize Transdermal Absorption Of Vitamin K1, Ramina Nabiee, Barent Dubois, Laura Green, Ajay Sharma, Siu Fun Wong, Hamidreza Montazeri Aliabadi 2018 Chapman University

In Vitro And Ex-Vivo Evaluation Of Topical Formulations Designed To Minimize Transdermal Absorption Of Vitamin K1, Ramina Nabiee, Barent Dubois, Laura Green, Ajay Sharma, Siu Fun Wong, Hamidreza Montazeri Aliabadi

Pharmacy Faculty Articles and Research

Topical application of Vitamin K1 has been demonstrated to effectively treat papulopustular skin rash, a serious and frequently encountered side effect of Epidermal Growth Factor Inhibitors (EGFRIs). Systemic absorption of vitamin K1 from skin and the resultant consequence of antagonizing EGFRIs anticancer effects jeopardizes the clinical acceptability of this rather effective treatment. The purpose of the present study was to rationally formulate and evaluate the release rate and transdermal absorption of a wide range of Vitamin K1 dermal preparations with a variety of physiochemical properties. A library of 33 formulations with were compounded and tested for Vitamin K1 permeation using ...


Polyrotaxane Variants And Their Effects On The Cholesterol Efflux In Patients Suffering From Niemann Pick Type C, Sydney Smith, Zach Struzik, David Thompson 2018 Purdue University

Polyrotaxane Variants And Their Effects On The Cholesterol Efflux In Patients Suffering From Niemann Pick Type C, Sydney Smith, Zach Struzik, David Thompson

The Summer Undergraduate Research Fellowship (SURF) Symposium

Niemann Pick type C disease (NPC) is a rare lysosomal storage disorder characterized by a progressive accumulation of cholesterol in the late endosomal/lysosomes compartment leading to cellular dysfunction and organ failure. Symptoms include ataxia, dysarthria, cognitive dysfunction, and seizures. Although average life expectancy is below 20, there are no FDA approved treatment available making it a serious unmet medical need. Clinical trials with 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD) has shown promise in cholesterol normalization within NPC cells. However, HP-beta-CD treatment has been shown to cause ototoxicity in NPC patients at high dosages. Supramolecular complexes known as polyrotaxanes have been synthesized in hopes ...


A V-To-F Substitution In Sk2 Channels Causes Ca2+ Hypersensitivity And Improves Locomotion In A C. Elegans Als Model, Young-Woo Nam, Sabia N. Baskoylu, Dimitris Gazgalis, Razan Orfali, Meng Cui, Anne C. Hart, Miao Zhang 2018 Chapman University

A V-To-F Substitution In Sk2 Channels Causes Ca2+ Hypersensitivity And Improves Locomotion In A C. Elegans Als Model, Young-Woo Nam, Sabia N. Baskoylu, Dimitris Gazgalis, Razan Orfali, Meng Cui, Anne C. Hart, Miao Zhang

Pharmacy Faculty Articles and Research

Small-conductance Ca2+-activated K+ (SK) channels mediate medium afterhyperpolarization in the neurons and play a key role in the regulation of neuronal excitability. SK channels are potential drug targets for ataxia and Amyotrophic Lateral Sclerosis (ALS). SK channels are activated exclusively by the Ca2+-bound calmodulin. Previously, we identified an intrinsically disordered fragment that is essential for the mechanical coupling between Ca2+/calmodulin binding and channel opening. Here, we report that substitution of a valine to phenylalanine (V407F) in the intrinsically disordered fragment caused a ~6 fold increase in the Ca2+ sensitivity of SK2-a channels. This substitution resulted in a ...


Photochemical Investigation Of High-Valent Metal-Oxo Intermediates Containing Corrole And Light-Harvesting Porphyrin Ligands, Jonathan Malone 2018 Western Kentucky University

Photochemical Investigation Of High-Valent Metal-Oxo Intermediates Containing Corrole And Light-Harvesting Porphyrin Ligands, Jonathan Malone

Masters Theses & Specialist Projects

In enzymatic and synthetic catalytic oxidations, high-valent iron-oxo intermediates play a vital role as the active oxidant. In this regard, many synthetic metal catalysts are designed as biomimetic models to resemble the active site of Cytochrome P450 enzymes (P450) which are the predominant oxidation catalysts in nature. Vitamin B12 cofactors, with a corrole-like structure corrin, are also utilized in some of the more difficult reactions in nature such as rearrangement and reductase reactions.

In this work, application of the promising photochemical method to corrolecontaining ligands systems showed much success in the generation of manganese(V)-oxo corrole intermediates using two ...


Design, Synthesis, And Evaluation Of Homochiral Peptides Containing Arginine And Histidine As Molecular Transporters, Naglaa Salem El-Sayed, Taryn Miyake, Amir Nasrolahi Shirazi, Shang Eun Park, Jimmy Clark, Stephani Buchholz, Keykavous Parang, Rakesh Tiwari 2018 Chapman University

Design, Synthesis, And Evaluation Of Homochiral Peptides Containing Arginine And Histidine As Molecular Transporters, Naglaa Salem El-Sayed, Taryn Miyake, Amir Nasrolahi Shirazi, Shang Eun Park, Jimmy Clark, Stephani Buchholz, Keykavous Parang, Rakesh Tiwari

Pharmacy Faculty Articles and Research

Linear (HR)n and cyclic [HR]n peptides (n = 4,5) containing alternate arginine and histidine residues were synthesized. The peptides showed 0–15% cytotoxicity at 5–100 μM in human ovarian adenocarcinoma (SK-OV-3) cells while they exhibited 0–12% toxicity in human leukemia cancer cell line (CCRF-CEM). Among all peptides, cyclic [HR]4 peptide was able to improve the delivery of a cell impermeable fluorescence-labeled phosphopeptide by two-fold. Fatty acids of different alkyl chain length were attached at the N-terminal of the linear peptide (HR)4 to improve the molecular transporter property. Addition of fatty acyl chains was expected ...


Efficient Intracellular Delivery Of Cell-Impermeable Cargo Molecules By Peptides Containing Tryptophan And Histidine, Amir Nasrolahi Shirazi, Saghar Mozaffari, Rinzhin Tshering Sherpa, Rakesh Tiwari, Keykavous Parang 2018 Chapman University

Efficient Intracellular Delivery Of Cell-Impermeable Cargo Molecules By Peptides Containing Tryptophan And Histidine, Amir Nasrolahi Shirazi, Saghar Mozaffari, Rinzhin Tshering Sherpa, Rakesh Tiwari, Keykavous Parang

Pharmacy Faculty Articles and Research

We have previously evaluated and reported numerous classes of linear and cyclic peptides containing hydrophobic and hydrophilic segments for intracellular delivery of multiple molecular cargos. Herein, a combination of histidine and tryptophan amino acids were designed and evaluated for their efficiency in intracellular delivery of cell-impermeable phosphopeptides and the anti-HIV drug, emtricitabine. Two new decapeptides, with linear and cyclic natures, both containing alternate tryptophan and histidine residues, were synthesized using Fmoc/tBu solid-phase chemistry. The peptides were characterized and purified by using matrix-assisted laser desorption/ionization (MALDI) spectroscopy and high-performance liquid chromatography (HPLC), respectively. These peptides did not show significant ...


Site-Selective Modification Of Peptides And Proteins Via Organocatalyzed Henry Reaction, Zilma Pereira Muneeswaran 2018 Seton Hall University

Site-Selective Modification Of Peptides And Proteins Via Organocatalyzed Henry Reaction, Zilma Pereira Muneeswaran

Seton Hall University Dissertations and Theses (ETDs)

In this research, peptides and protein containing serine on the N-terminus underwent site-selective modification following organocatalyzed bioconjugation that offered an additional functional group. It was shown that transforming the N-terminus serine to an aldehyde allowed site-specific bioconjugation to occur by utilizing the well-known Henry reaction. This method also grants a safer pathway for bioconjugation utilizing “green-chemistry” and biocompatible conditions. Amino acids and amino acid derived organocatalysts were utilized in the Henry reaction resulting in yields of up to 86 % conversion. Promising preliminary results were achieved in this research using peptides and myoglobin as the bioconjugation targets. Further investigation to be ...


Development Of Lc-Ms For The Identification And Characterization Of Non-Adjacent Dna Photoproduct Formation In G-Quadruplex Forming Sequences, Claudia Posadas 2018 Washington University in St. Louis

Development Of Lc-Ms For The Identification And Characterization Of Non-Adjacent Dna Photoproduct Formation In G-Quadruplex Forming Sequences, Claudia Posadas

Arts & Sciences Electronic Theses and Dissertations

Ultraviolet light is well known to induce cyclobutane pyrimidine dimers (CPD) and pyrimidine (6–4) pyrimidone photoproducts in duplex DNA, which interfere with DNA replication and transcription. Recently, a new class of DNA photoproducts known as anti cyclobutanepyrimidine dimers have been discovered, which form in G-quadruplex forming sequences in solution. G-quadruplex structures have been proposed to form in human DNA telomeres and certain promoters in vivo but evidence for their existence has been lacking. Since anti-cyclobutante pyrimidine dimers have been shown to form in G-quadruplex forming sequences, their formation in irradiated human cells could be used to confirm the ...


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

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 ...


Catalyzed And Uncatalyzed Modifications Of Nucleosides, Synthesis Of Hippadine, And Deuterated 1,2,3-Triazoles, Hari K. Akula 2018 The Graduate Center, City University of New York

Catalyzed And Uncatalyzed Modifications Of Nucleosides, Synthesis Of Hippadine, And Deuterated 1,2,3-Triazoles, Hari K. Akula

All Dissertations, Theses, and Capstone Projects

The C4 amide carbonyl of O-t-butyldimethylsilyl-protected thymidine, 2’-deoxyuridine, and 3’-azidothymidine (AZT) was activated by reaction with (benzotriazol-1-yloxy)tris(dimethylamino) phosphonium hexafluorophosphate (BOP) and 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) in THF as solvent. This led to the formation of corresponding O4-(benzotriazol-1-yl) derivatives, which are reactive intermediates. Substitution at the C4 position was then carried out by reactions with alkyl and aryl amines, and thiols. Typically, reactions were conducted as a two-step, one-pot transformation, and also as a one-step conversion. After examining the reactions, the formation of 1-(4-pyrimidinyl)-1H-benzotriazole-3-oxide derivatives from the ...


Towards The Development Of A Novel Dna Binding Fluorescent Cell Stain; An Analysis Of Common Dna Dyes And Their Applications, Lauren Kapteyn 2018 Liberty University

Towards The Development Of A Novel Dna Binding Fluorescent Cell Stain; An Analysis Of Common Dna Dyes And Their Applications, Lauren Kapteyn

Senior Honors Theses

Fluorescent deoxyribonucleic acid (DNA) stains that permeate cells are used to observe cellular processes in vivo, making them valuable tools. For the proposal of a new stain, ethidium bromide, cyanine dyes, Hoechst stains, macarpine, DAPI and DRAQ5 are first examined. Features contributing to DNA binding mechanism, toxicity, and cell membrane transport are analyzed for these compounds. The mechanism of DNA binding contributes to the toxicity of the compound. For dyes with well-understood transport mechanisms, multi-drug protein transporters are vital players, though this remains an area for ongoing research as many mechanisms are not well studied. A novel anthraquinone-based compound is ...


Novel Combination Bmp7 And Hgf Gene Therapy Instigates Selective Myofibroblast Apoptosis And Reduces Corneal Haze In Vivo, Suneel Gupta, Michael K. Fink, Arkasubhra Ghosh, Ratnakar Tripathi, Prashant R. Sinha, Ajay Sharma, Nathan P. Hesemann, Shyam S. Chaurasia, Elizabeth A. Giuliano, Rajiv R. Mohan 2018 Harry S. Truman Memorial Veterans’ Hospital

Novel Combination Bmp7 And Hgf Gene Therapy Instigates Selective Myofibroblast Apoptosis And Reduces Corneal Haze In Vivo, Suneel Gupta, Michael K. Fink, Arkasubhra Ghosh, Ratnakar Tripathi, Prashant R. Sinha, Ajay Sharma, Nathan P. Hesemann, Shyam S. Chaurasia, Elizabeth A. Giuliano, Rajiv R. Mohan

Pharmacy Faculty Articles and Research

PURPOSE. We tested the potential of bone morphogenic protein 7 (BMP7) and hepatocyte growth factor (HGF) combination gene therapy to treat preformed corneal fibrosis using established rabbit in vivo and human in vitro models.

METHODS. Eighteen New Zealand White rabbits were used. Corneal fibrosis was produced by alkali injury. Twenty-four hours after scar formation, cornea received topically either balanced salt solution (BSS; n ¼ 6), polyethylenimine-conjugated gold nanoparticle (PEI2-GNP)-naked plasmid (n ¼ 6) or PEI2-GNP plasmids expressing BMP7 and HGF genes (n ¼ 6). Donor human corneas were used to obtain primary human corneal fibroblasts and myofibroblasts for mechanistic ...


Recently Discovered Benzo(A)Pyrene Induced Health Effects And Their Threat To The Inland Empire, Quinn Navarro 2018 University of Redlands

Recently Discovered Benzo(A)Pyrene Induced Health Effects And Their Threat To The Inland Empire, Quinn Navarro

Armacost Library Undergraduate Research Award (ALURA)

This study investigated recent discoveries of Benzo(a)Pyrene (BaP) in order to determine the current threat BaP poses to residents of Southern California. Literature reviews comprise the research done on BaP-induced health effects. Primary articles reviewed include “Adverse Effect of Sub-Chronic Exposure to Benzo(a)Pyrene and Protective Effect of Butylated Hydroxyanisole on Learning and Memory Ability in Male

Sprague-Dawley Rat” by Xiao Liang (2014), and “Bioaccumulation and oxidative damage in juvenile scallop Chlamys farreri exposed to benzo[a]Pyrene, benzo[b]Fluoranthene and chrysene” by Meng Xiu (2014). These studies conclude that BaP potentially impairs memory and learning ...


The Generation Of Three Novel Aspirin Co-Crystals, Olivia Ray 2018 University of Iowa

The Generation Of Three Novel Aspirin Co-Crystals, Olivia Ray

University of Iowa Honors Theses

We report the discovery of three co-crystals of acetylsalicylic acid (ASA). The co-crystals include different co-crystal formers (CCFs) containing pyridine moieties: 4,4’-bipyridine (4,4’-bipy), 4,4'-butane-1,4-diyldipyridine (4,4’-butane), and trans-bis(4-pyridyl)poly-2-ene (4-pyr-poly-2-ene). The three co-crystals are 2(ASA)·(4,4’-bipy), 2(ASA)·(4,4’-butane), and 2(ASA)·(4-pyr-poly-2-ene). All the co-crystals were formed by rapid solvent evaporation of diethyl ether. 2(ASA)·(4,4’-bipy) was also formed using dry grinding. The three co-crystals consist of three-component hydrogen-bonded assemblies held together by O-H···N hydrogen bonds. Both 2(ASA)·(4,4 ...


Nicotine Administration And Withdrawal And Its Effect On Sleep Latency, Relevant Sleep Variables, And Endogenous Corticosterone Levels In Mice, Vishnu Iyer 2018 University of Colorado, Boulder

Nicotine Administration And Withdrawal And Its Effect On Sleep Latency, Relevant Sleep Variables, And Endogenous Corticosterone Levels In Mice, Vishnu Iyer

Undergraduate Honors Theses

NREM and REM sleep have shown an exceptional importance in controlling various cognitive functions (Brown et al, 2012), and disruption of such sleep states can cause mental and physical impairments (Christie et al, 2008). Disruptions in sleep stages (Wakefulness, REM, NREM) can be identified via EEG recordings in mice without much interference (Mckenna et al, 2008). Circadian Rhythm, hormonal markers, and stress all affect the duration, intensity and timing of these sleep stages (Brown et al, 2004; Veasey et al 2004; Christie et al, 2008). One cohort of mice (n=7) underwent a baseline condition (BL), a nicotine administration condition ...


Discovery Of Bioactive Natural Products From Sugarcane, Rory Patrick Taylor 2018 Southern Cross University

Discovery Of Bioactive Natural Products From Sugarcane, Rory Patrick Taylor

Theses

This research was undertaken to discover new potential products (with a focus on flavonoids) from sugarcane and sugar production by-products that have pharmaceutical, nutraceutical or functional food applications. Specifically, cytotoxic, antioxidant, anti-inflammatory/immune modulation and glycaemic index (GI) activities were surveyed. The results suggest that there are potentially novel anti-inflammatory and α-amylase inhibiting compound(s) present. These extracts or compounds may have use in the treatment of diabetes mellitus type 2 or inflammation-related diseases such as arthritis, multiple sclerosis and atherosclerosis. Further research such as compound identification and in vivo testing is warranted.


Synthesis And Electrical Properties Of Copolymers Containing 3-Phenyl[5]Ferrocenophane-1,5-Dimethylene And Vinylimidazole, Muteb H. Alshammari 2017 Pittsburg State University

Synthesis And Electrical Properties Of Copolymers Containing 3-Phenyl[5]Ferrocenophane-1,5-Dimethylene And Vinylimidazole, Muteb H. Alshammari

Electronic Thesis Collection

Ferrocene is a well-known organometallic compound and its structure consists of an iron atom sandwiched between two cyclopentadienyl rings. Ferrocene has unique properties such as redox chemistry, high electron density, thermal stability and aromaticity. In addition, the ferrocene can be incorporated into polymers either into the backbone or on the side chains. Ferrocene incorporated polymers have received considerable attention in the areas of electro-catalysis, electrode coating, and battery applications. Therefore, the main purpose of this study is to characterize the electrochemical behavior of copolymers of 3-phenyl[5]ferrocenophane-1,5-dimethylene with vinyl imidazole in aqueous solutions with various electrolytes: sodium perchlorate ...


Sodium Channel Nav1.3 Is Important For Enterochromaffin Cell Excitability And Serotonin Release, Peter R. Strege, Kaitlyn Knutson, Samuel J. Eggers, Joyce H. Li, Fan Wang, David Linden, Joseph H. Szurszewski, Lorin Milescu, Andrew B. Leiter, Gianrico Farrugia, Arthur Beyder 2017 Mayo Clinic

Sodium Channel Nav1.3 Is Important For Enterochromaffin Cell Excitability And Serotonin Release, Peter R. Strege, Kaitlyn Knutson, Samuel J. Eggers, Joyce H. Li, Fan Wang, David Linden, Joseph H. Szurszewski, Lorin Milescu, Andrew B. Leiter, Gianrico Farrugia, Arthur Beyder

Open Access Articles

In the gastrointestinal (GI) epithelium, enterochromaffin (EC) cells are enteroendocrine cells responsible for producing > 90% of the body's serotonin (5-hydroxytryptamine, 5-HT). However, the molecular mechanisms of EC cell function are poorly understood. Here, we found that EC cells in mouse primary cultures fired spontaneous bursts of action potentials. We examined the repertoire of voltage-gated sodium channels (NaV) in fluorescence-sorted mouse EC cells and found that Scn3a was highly expressed. Scn3a-encoded NaV1.3 was specifically and densely expressed at the basal side of both human and mouse EC cells. Using electrophysiology, we found that EC cells expressed robust NaV1.3 ...


Difatty Acyl-Conjugated Linear And Cyclic Peptides For Sirna Delivery, Hung Do, Meenakshi Sharma, Naglaa Salem El-Sayed, Parvin Mahdipoor, Emira Bousoik, Keykavous Parang, Hamidreza Montazeri Aliabadi 2017 Chapman University

Difatty Acyl-Conjugated Linear And Cyclic Peptides For Sirna Delivery, Hung Do, Meenakshi Sharma, Naglaa Salem El-Sayed, Parvin Mahdipoor, Emira Bousoik, Keykavous Parang, Hamidreza Montazeri Aliabadi

Pharmacy Faculty Articles and Research

A number of amphiphilic difatty acyl linear and cyclic R5K2 peptide conjugates were synthesized by solid-phase peptide methods to enhance the interaction with the hydrophobic cellular phospholipid bilayer and to improve siRNA delivery and silencing. Binding to siRNA molecules was significantly less for the cyclic peptide conjugates. A gradual decrease was observed in the particle size of the complexes with increasing peptide/siRNA ratio for most of the synthesized peptides, suggesting the complex formation. Most of the complexes showed a particle size of less than 200 nm, which is considered an appropriate size for in vitro siRNA delivery. A number ...


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 ...


Digital Commons powered by bepress