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Medicinal-Pharmaceutical Chemistry Commons

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Interactions Of Carbohydrate-Conjugated Nanoparticles With Mycobacterium Smegmatis, Kalana W. Jayawardana, H. Surangi N. Jayawardena, Thareendra De Zoysa, Mingdi Yan 2014 University of Massachusetts Lowell

Interactions Of Carbohydrate-Conjugated Nanoparticles With Mycobacterium Smegmatis, Kalana W. Jayawardana, H. Surangi N. Jayawardena, Thareendra De Zoysa, Mingdi Yan

UMass Center for Clinical and Translational Science Research Retreat

Mycobacterium smegmatis is a non-pathogenic microorganism and has been widely used as a model organism to study infections caused by M. tuberculosis and other mycobacterial pathogens. We report that nanoparticles conjugated with selected carbohydrate show a striking increase in the surface adherence by M. smegmatis. This applies to silica nanoparticles and magnetic nanoparticles ranging from 100 nm to 5 nm. Under the same experimental conditions, minimum adhesion was observed for unfunctionalized nanoparticles. The synthesis and characterization of the glyconanoparticles will be presented. The finding is applied to imaging M. smegmatis infected lung epithelial cells, and the results will be discussed.


Branching Into Rnai: Synthesis, Characterization And Biology Of Branch And Hyperbranch Sirnas, Anthony Muriithi Maina 2014 Seton Hall University

Branching Into Rnai: Synthesis, Characterization And Biology Of Branch And Hyperbranch Sirnas, Anthony Muriithi Maina

Seton Hall University Dissertations and Theses (ETDs)

The cancer epidemic continues to afflict millions of humans world-wide each year and despite a renewed hope with the development of new and improved forms of therapy, a cure for cancer remains an elusive goal. This is partly related to the rise of resilient forms of tumors that have evolved with resistance towards conventional chemotherapy and radiation treatments. Moreover, these non-specific therapeutic regimens are highly toxic, leading to severe immunosuppressive effects which poisons the body and compromises the road towards remission. In an effort to mitigate these limitations, cancer-targeting approaches are currently experiencing a renaissance in the translation of new ...


Design, Synthesis And Biological Evaluation Of Novel Compounds With Cns-Activity Targeting Cannabinoid And Biogenic Amine Receptors, Alexander M. Sherwood 2014 University of New Orleans

Design, Synthesis And Biological Evaluation Of Novel Compounds With Cns-Activity Targeting Cannabinoid And Biogenic Amine Receptors, Alexander M. Sherwood

University of New Orleans Theses and Dissertations

This work seeks to contribute to the discipline of neuropharmacology by way of structure activity relationship from the standpoint of an organic chemist. More specifically, we sought to develop robust synthetic methodology able to efficiently produce an array of compounds for the purpose of systematic evaluation of their interaction with specific sights within the central nervous system (CNS) in order to better understand the mind and to develop drugs that may have beneficial effects on neurological function.

The focus of these studies has been toward the development of novel molecules, using a structure-activity relationship approach, that exhibit binding affinity at ...


Cu (Ii) Catalyzed Gateways In The Synthesis Of Acridine Derivatives And Their Biological Evaluation As Anti-Cancer Drugs, Rajesh Komati 2014 Rajesh Komati

Cu (Ii) Catalyzed Gateways In The Synthesis Of Acridine Derivatives And Their Biological Evaluation As Anti-Cancer Drugs, Rajesh Komati

University of New Orleans Theses and Dissertations

Telomeres are nucleoprotein complexes found at the ends of linear eukaryotic chromosomes. Telomeres consist of a short sequence of repetitive double stranded DNA, TTAGGG repeats in humans (and all mammals), and a complex of 6 proteins, termed the shelterin complex. The length of the telomeres varies greatly between species, from approximately 300 base pairs in yeast to many 10-15 kilo bases in humans, because of the end replication problem this length get shorten with each cell division and ultimately leads to cell death. However the immortal eukaryotic cells and some transformed human cells over come this incomplete end replication problem ...


Metal Stopping Reagents Facilitate Discontinuous Activity Assays Of The De Novo Purine Biosynthesis Enzyme Pure, Kelly L. Sullivan, Loredana C. Huma, Elwood Mullins, Michael E. Johnson, T. Joseph Kappock 2014 Purdue University

Metal Stopping Reagents Facilitate Discontinuous Activity Assays Of The De Novo Purine Biosynthesis Enzyme Pure, Kelly L. Sullivan, Loredana C. Huma, Elwood Mullins, Michael E. Johnson, T. Joseph Kappock

Department of Biochemistry Faculty Publications

The conversion of 5-aminoimidazole ribonucleotide (AIR) to 4-carboxy-AIR (CAIR) represents an unusual divergence in purine biosynthesis: microbes and nonmetazoan eukaryotes use class I PurEs while animals use class II PurEs. Class I PurEs are therefore a potential antimicrobial target; however, no enzyme activity assay is suitable for high throughput screening (HTS). Here we report a simple chemical quench that fixes the PurE substrate/product ratio for 24 h, as assessed by the Bratton-Marshall assay (BMA) for diazotizable amines. The ZnSO4 stopping reagent is proposed to chelate CAIR, enabling delayed analysis of this acid-labile product by BMA or other HTS ...


Radiopharmaceuticals: The Application Of Technetium-99m And Rhenium Complexes, Angela Kristin Binion 2014 Syracuse University

Radiopharmaceuticals: The Application Of Technetium-99m And Rhenium Complexes, Angela Kristin Binion

Syracuse University Honors Program Capstone Projects

Nuclear imaging used in diagnostic medicine requires the use of radiopharmaceuticals to make biological areas visible under a gamma camera. Although much success has been found in the use of technetium based imaging agents, their corresponding rhenium complexes can provide insight into the chemical properties of these radiopharmaceuticals without the potentially damaging effects of radiation. Technetium and rhenium complexes utilize a bifunctional chelator to act as a linker between biological vectors and the metal, improving the coordination between the two. Ligands containing thiazole rings have been successfully coordinated to technetium or rhenium tricarbonyl complexes, although it is uncertain whether coordination ...


Drug Screening Target For Alzheimer's Disease And Method Of Screening Potential Drugs, Joseph Audie, Sergei Y. Ponomarev 2014 Sacred Heart University

Drug Screening Target For Alzheimer's Disease And Method Of Screening Potential Drugs, Joseph Audie, Sergei Y. Ponomarev

Chemistry & Physics Faculty Publications

Drug screening targets and method of screening for potential drugs for treatment or amelioration of Alzheimer's Disease are provided.


Syntheses Of Precursors To Fluorine-18 Labeled Pet Imaging Agents, Lindsay B. Boling 2014 University of Tennessee - Knoxville

Syntheses Of Precursors To Fluorine-18 Labeled Pet Imaging Agents, Lindsay B. Boling

Chancellor’s Honors Program Projects

No abstract provided.


Functionalization And Modification Of Naphthaquinone Analogs As Her2 Kinase Inhibitors, Divya Jyothi Lella 2014 Western Kentucky University

Functionalization And Modification Of Naphthaquinone Analogs As Her2 Kinase Inhibitors, Divya Jyothi Lella

Masters Theses & Specialist Projects

HER2 overexpression in breast cancer tumors predicts lower overall survival. Because of the aggressive nature of HER2 tumors and the association with metastatic disease, the HER2 receptor holds great promise as a therapeutic target in metastatic breast cancer. We are developing small molecule inhibitors that bind to the ATP binding site of the tyrosine kinase domain in order to inhibit tyrosine auto-phosphorylation. This process controls biological pathways that mediate the cell growth. In normal cells this process is highly controlled. We are targeting the modification of the side chain of the hydroxy methyl group of 2-Hydroxy methyl-5,8-dimethoxy-1,4-naphthaquinone. These ...


Green's Functions Of Discrete Fractional Calculus Boundary Value Problems And An Application Of Discrete Fractional Calculus To A Pharmacokinetic Model, Sutthirut Charoenphon 2014 Western Kentucky University

Green's Functions Of Discrete Fractional Calculus Boundary Value Problems And An Application Of Discrete Fractional Calculus To A Pharmacokinetic Model, Sutthirut Charoenphon

Masters Theses & Specialist Projects

Fractional calculus has been used as a research tool in the fields of pharmacology, biology, chemistry, and other areas [3]. The main purpose of this thesis is to calculate Green's functions of fractional difference equations, and to model problems in pharmacokinetics. We claim that the discrete fractional calculus yields the best prediction performance compared to the continuous fractional calculus in the application of a one-compartmental model of drug concentration. In Chapter 1, the Gamma function and its properties are discussed to establish a theoretical basis. Additionally, the basics of discrete fractional calculus are discussed using particular examples for further ...


Selective Oxidations By Metalloporphyrins And Metallocorroles, Tse-Hong Chen 2014 Western Kentucky University

Selective Oxidations By Metalloporphyrins And Metallocorroles, Tse-Hong Chen

Masters Theses & Specialist Projects

Highly reactive transition metal-oxo intermediates are important active oxidant involved in numerous enzymes such as cytochrome P450 monooxygenases as well as in many useful metal-catalyzed oxidations. Many transition metal catalysts are designed for biomimetic studies of the predominant oxidation catalysts in Nature, the cytochrome P450 enzymes. In this work, a series of metalloporphyrin and metallocorrole complexes have been successfully synthesized and spectroscopically characterized by UV-vis, GCMS and 1H-NMR. The utilization of these complexes as catalysts for selective oxidation of sulfides and photocatalytic aerobic oxidations of activated hydrocarbons were investigated. Ruthenium(II) porphyrin complexes (2) and iron(III) corrole complexes ...


Peptidomimetic Ghs-R1a Agonists As Pet Imaging Agents For Prostate Cancer, Milan M. Fowkes 2014 The University of Western Ontario

Peptidomimetic Ghs-R1a Agonists As Pet Imaging Agents For Prostate Cancer, Milan M. Fowkes

Electronic Thesis and Dissertation Repository

Contemporary diagnostic techniques for prostate cancer (PCa) have a limited ability to distinguish between benign and malignant disease. The ghrelin receptor has a differential expression in normal, benign and cancerous prostatic tissue. Targeting this receptor with 18F-radiolabelled peptidomimetics would enable differentiation between these disease states via PET imaging. A series of 19F-peptidomimetics were synthesized and characterized by HRMS, HPLC and 1 H-NMR spectroscopy in order to test locations for 18F radioisotope insertion. Competitive receptor binding assays using HEK293/GHS-R1a cells were used to evaluate compound binding affinities. This led to the identification of two lead compounds: [1-Nal4,Lys5(4-FB)]G-7039 ...


Synthesis Of Thiophene Analogs As Potential Antagonists Of Chemokine Receptor Type 4 (Cxcr4), Francisco Javier Garcia Jr. 2014 Georgia State University

Synthesis Of Thiophene Analogs As Potential Antagonists Of Chemokine Receptor Type 4 (Cxcr4), Francisco Javier Garcia Jr.

Georgia State Undergraduate Research Conference

No abstract provided.


Speciation, Metabolism, Toxicity, And Protein-Binding Of Different Arsenic Species In Human Cells, Szabina A. Stice 2014 Florida International University

Speciation, Metabolism, Toxicity, And Protein-Binding Of Different Arsenic Species In Human Cells, Szabina A. Stice

FIU Electronic Theses and Dissertations

Despite of its known toxicity and potential to cause cancer, arsenic has been proven to be a very important tool for the treatment of various refractory neoplasms. One of the promising arsenic-containing chemotherapeutic agents in clinical trials is Darinaparsin (dimethylarsinous glutathione, DMAIII(GS)). In order to understand its toxicity and therapeutic efficacy, the metabolism of Darinaparsin in human cancer cells was evaluated. With the aim of detecting all potential intermediates and final products of the biotransformation of Darinaparsin and other arsenicals, an analytical method employing high performance liquid chromatography inductively coupled mass spectrometry (HPLC-ICP-MS) was developed. This method was ...


Synthesis And Functionalization Of Virus-Mimicking Cationic Block Copolymers With Pathogen-Associated Carbohydrates As Potential Vaccine Adjuvants, J. R. Adams, M. Goswami, N. L.B. Pohl, Surya K. Mallapragada 2014 Iowa State University

Synthesis And Functionalization Of Virus-Mimicking Cationic Block Copolymers With Pathogen-Associated Carbohydrates As Potential Vaccine Adjuvants, J. R. Adams, M. Goswami, N. L.B. Pohl, Surya K. Mallapragada

Chemical and Biological Engineering Publications

We report the synthesis of a family of amphiphilic pentablock polymers with different cationic blocks and with controlled architectures as potential vaccine carriers for subunit vaccines. The temperature and pH-dependent micellization and gelation of these pentablock copolymers can provide a depot for sustained protein and gene delivery. The amphiphilic central triblock promotes cellular endocytosis, good gene delivery and has been used effectively as a vaccine adjuvant. The pentablock copolymer outer blocks condense DNA spontaneously as a result of electrostatic interactions for sustained combinational therapy. This family of polymers with different cationic groups was evaluated based on DNA complexation-ability and cytotoxicity ...


Identification Of Tetrapeptides From A Mixture Based Positional Scanning Library That Can Restore Nm Full Agonist Function Of The L106p, I69t, I102s, A219v, C271y, And C271r Human Melanocortin-4 Polymorphic Receptors (Hmc4rs), Erica M. Haslach, Huisuo Huang, Marvin Dirain, Ginamarie Debevec, Phaedra Geer, Radleigh Santos, Marc Giulianotti, Clemencia Pinilla, Jon R. Appel, Skye R. Doering, Michael A. Walters, Richard A. Houghten, Carrie Haskell-Luevano 2014 University of Florida

Identification Of Tetrapeptides From A Mixture Based Positional Scanning Library That Can Restore Nm Full Agonist Function Of The L106p, I69t, I102s, A219v, C271y, And C271r Human Melanocortin-4 Polymorphic Receptors (Hmc4rs), Erica M. Haslach, Huisuo Huang, Marvin Dirain, Ginamarie Debevec, Phaedra Geer, Radleigh Santos, Marc Giulianotti, Clemencia Pinilla, Jon R. Appel, Skye R. Doering, Michael A. Walters, Richard A. Houghten, Carrie Haskell-Luevano

Mathematics Faculty Articles

Human obesity has been linked to genetic factors and single nucleotide polymorphisms (SNPs). Melanocortin-4 receptor (MC4R) SNPs have been associated with up to 6% frequency in morbidly obese children and adults. A potential therapy for individuals possessing such genetic modifications is the identification of molecules that can restore proper receptor signaling and function. These compounds could serve as personalized medications improving quality of life issues as well as alleviating diseases symptoms associated with obesity including type 2 diabetes. Several hMC4 SNP receptors have been pharmacologically characterized in vitro to have a decreased, or a lack of response, to endogenous agonists ...


Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres 2014 University of Massachusetts - Amherst

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 ...


Expression And Characterization Of The Novel Oxidase Virh-Ox, John Dronzek 2014 Connecticut College

Expression And Characterization Of The Novel Oxidase Virh-Ox, John Dronzek

Chemistry Honors Papers

No abstract provided.


Science Classics, Mark Masthay 2014 University of Dayton

Science Classics, Mark Masthay

Chemistry Faculty Publications

An essay on the impact of the works in the Imprints and Impressions: Milestones in Human Progress, an exhibition of rare books from the collection of Stuart Rose. Exhibition was held Sept. 29-Nov. 9, 2014, at the University of Dayton.


Dj-1 And Atp13a2: Two Proteins Involved In Parkinson’S Disease, Josephat M Asiago 2014 Purdue University

Dj-1 And Atp13a2: Two Proteins Involved In Parkinson’S Disease, Josephat M Asiago

Open Access Dissertations

Parkinson's disease (PD) is the second most common neurodegenerative disorder after Alzheimer's disease, affecting approximately 0.3% of the total U.S. population, and its prevalence increases with age. Two neuropathological hallmarks of PD are the loss of dopaminergic neurons in the substantia nigra pars compacta, a region in the midbrain involved in initiating and sustaining movement, and the presence of cytosolic inclusions called Lewy bodies (LBs) in various brain regions. LBs are enriched with fibrillar forms of the presynaptic protein &agr;-synuclein (aSyn). Two autosomal recessive genes implicated in familial PD are PARK9, encoding the P-type ATPase ATP13A2 ...


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