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Rnai Nanotechnology: A Platform For Sirna Screening And Cancer Gene Therapy, Mayurbhai Ravikant Patel 2016 Seton Hall University

Rnai Nanotechnology: A Platform For Sirna Screening And Cancer Gene Therapy, Mayurbhai Ravikant Patel

Seton Hall University Dissertations and Theses (ETDs)

Over the past two decades, advances in RNA structural biology have improved our understanding of the structures and folding properties of naturally occurring RNAs. RNA sequences and structures participate in many specific biological functions, such as those performed by messenger RNA (mRNA), ribosomal RNA (rRNA), transfer RNA (tRNA), micro RNA (miRNA), short-interfering RNA (siRNA), small nuclear RNA (snRNA) and many others. The noncoding RNAs, such as siRNA, do not express proteins but have been utilized in a wide range of applications, including RNA interference (RNAi) and the regulation of mRNA expression. These important biological functions have been implemented in gene ...


Repeated Zolpidem Treatment Effects On Sedative Tolerance, Withdrawal, Mrna Levels, And Protein Expression, Brittany T. Wright 2016 University of Tennessee Health Science Center

Repeated Zolpidem Treatment Effects On Sedative Tolerance, Withdrawal, Mrna Levels, And Protein Expression, Brittany T. Wright

Theses and Dissertations (ETD)

Zolpidem and benzodiazepines (BZs) potentiate the inhibitory action of gamma-Aminobutyric acid (GABA) by allosterically binding to GABAA receptors (GABAAR). Prolonged use of GABAAR positive allosteric modulators (PAM) can lead to behavioral tolerance, the diminished response to the same drug dose with repeated use, and withdrawal, a group of symptoms that occur due to abrupt end of drug treatment. Zolpidem is a short-acting, non-BZ GABAAR PAM whose potential for tolerance and withdrawal is unclear. Zolpidem demonstrates sedative efficacy similar to BZs and has become a main treatment of insomnia in lieu of BZs. Zolpidem replaced BZs due to lower incidences of ...


Antibiotic Drug Discovery With An Eye Towards Overcoming Drug Resistance, Daniel Towner Hoagland 2016 University of Tennessee Health Science Center

Antibiotic Drug Discovery With An Eye Towards Overcoming Drug Resistance, Daniel Towner Hoagland

Theses and Dissertations (ETD)

As a species, humans have become ever reliant on the use of antibiotics to facilitate our everyday lives. The widespread emergence of resistance to currently used antibiotics is commonly attributed to an over use in our society. Such resistance, coupled with a lack of innovation and production of novel antibiotic drugs, threatens to return humanity to an era similar to one before the discovery of the first antibiotics. The need to find new agents to be used in this fight is paramount, as well as learning from our recent failures to produce such compounds. This document will highlight my efforts ...


Incidence Of Hypomagnesemia On Proton Pump Inhibitors At The Huntington Veterans Affairs Medical Center – Ihop, Ebrahim Sabbagh, DO, Chelsey R. Houchins, James Allman, II, PharmD, Samson Teka, MD 2016 Marshall University

Incidence Of Hypomagnesemia On Proton Pump Inhibitors At The Huntington Veterans Affairs Medical Center – Ihop, Ebrahim Sabbagh, Do, Chelsey R. Houchins, James Allman, Ii, Pharmd, Samson Teka, Md

Marshall Journal of Medicine

Abstract

Title: Incidence of hypomagnesemia on proton pump inhibitors at the Huntington Veterans Affairs Medical Center – IHOP

Purpose:

Proton pump inhibitors (PPIs), both prescription and over-the-counter, are widely used for the treatment of acid-related disease states such as dyspepsia, gastroesophageal reflex disease, esophagitis, and peptic ulcers. These medications are generally considered safe in most patient populations; however, there are several adverse effects that may occur with long-term use. Hypomagnesemia is a newer complication arising in the literature following multiple case reports over the past several years, although the true incidence of hypomagnesemia associated with PPI use remains unclear at this ...


Determination Of Isotopic Abundance Of 13c/12c Or 2h/1h And 18o/16o In Biofield Energy Treated 1-Chloro-3-Nitrobenzene (3-Cnb) Using Gas Chromatography-Mass Spectrometry, Mahendra Kumar Trivedi 2016 Selected Works

Determination Of Isotopic Abundance Of 13c/12c Or 2h/1h And 18o/16o In Biofield Energy Treated 1-Chloro-3-Nitrobenzene (3-Cnb) Using Gas Chromatography-Mass Spectrometry, Mahendra Kumar Trivedi

Mahendra Kumar Trivedi

1-Chloro-3-nitrobenzene (3-CNB) is an aromatic halo-amine compound used as chemical intermediate for the production of several fine chemicals like pharmaceuticals, dyes, agricultural chemicals, etc. The stable isotope ratio analysis has drawn attention in numerous fields such as agricultural, food authenticity, biochemistry, etc. The objective of the current research was to investigate the impact of the biofield energy treatment on the isotopic abundance ratios of PM+1/PM, PM+2/PM and PM+3/PM in 3-CNB using gas chromatography - mass spectrometry (GC-MS). The sample, 3-CNB was divided into two parts - one part was denoted as control and another part was ...


Crystal Protein Cry5b As A Novel And Powerful Anthelmintic, David Koch, Zeynep Mirza, Yan Hu, Thanh-thanh Nguyen, Gary R. Ostroff, Raffi V. Aroian 2016 University of Massachusetts Medical School

Crystal Protein Cry5b As A Novel And Powerful Anthelmintic, David Koch, Zeynep Mirza, Yan Hu, Thanh-Thanh Nguyen, Gary R. Ostroff, Raffi V. Aroian

UMass Center for Clinical and Translational Science Research Retreat

Soil-transmitted helminths (STHs), most notably, hookworms, whipworms, and Ascaris, are nematodes that infect more than 1.5 billion of the poorest people and are amongst the leading causes of morbidity worldwide. Only two classes of de-worming drugs (anthelmintics) are available for treatment, and only one is commonly used in mass drug administrations. New anthelmintics are urgently needed to overcome emerging resistance and to produce higher cure rates. Crystal (Cry) proteins, in particular Cry5B, made by Bacillus thuringiensis (Bt) are promising new candidates. Cry5B has excellent anthelmintic properties against many free-living and parasitic nematodes, including in vivo efficacy against multiple STH ...


Theoretical And Experimental Analysis Of The Antioxidant And Anti-Amyloid Features Of Synthetic Resveratrol Mimics, William Horton, Anne Kokel, Fanni Török, Chris Tran, Marianna Török, Bela Török 2016 University of Massachusetts Boston

Theoretical And Experimental Analysis Of The Antioxidant And Anti-Amyloid Features Of Synthetic Resveratrol Mimics, William Horton, Anne Kokel, Fanni Török, Chris Tran, Marianna Török, Bela Török

UMass Center for Clinical and Translational Science Research Retreat

Diaryl hydrazones, possessing similar structure to the popular red wine antioxidant resveratrol, have been previously identified as multitarget compounds interfering with several processes associated with the pathogenesis of Alzheimer’s disease (AD). These compounds exhibited particularly strong inhibition of the amyloid beta (A) peptide self-assembly, including blocking the formation of fibrils and oligomers, species that are widely accepted to be neurotoxic. The molecules were also powerful free radical scavengers and thus have a potential to defend against oxidative stress.

In order to learn more about the mode of action of the compounds, theoretical and experimental studies have been carried out ...


Invitrometrix Qcm-Based Cell Biosensor: Research Tool To Accelerate Pharmaceutical Drug Discovery Success, Abiche H. Dewilde 2016 University of Massachusetts Lowell

Invitrometrix Qcm-Based Cell Biosensor: Research Tool To Accelerate Pharmaceutical Drug Discovery Success, Abiche H. Dewilde

UMass Center for Clinical and Translational Science Research Retreat

As part of the mini-symposium entitled "Shark Tank-UMass Spin-out Life Sciences Start-ups," Dr. Dewilde discusses an example of UMass life sciences technology that has been spun out into a start-up company -- Cell QCM from UMass Lowell.


Hit Identification For Pkcζ Inhibitors: Structure-Based Optimization, Virtual Screening, And Biological Evaluation, Xiaoxin Wu 2016 University of Tennessee Health Science Center

Hit Identification For Pkcζ Inhibitors: Structure-Based Optimization, Virtual Screening, And Biological Evaluation, Xiaoxin Wu

Theses and Dissertations (ETD)

Protein kinase C ζ (PKCζ) is believed to be a promising target for the treatment of some diseases, including inflammatory diseases, obesity and diabetes. Hit identification of PKCζ inhibitors was conducted by structure-based modification, virtual screening and biological evaluation. Among all the compounds selected and synthesized, compound JW-1-60A showed moderate activity against PKCζ at 30 μM and 100 μM. The molecular modeling studies showed that the binding mode of JW-1-61A was very close to the binding mode of JP-3-149, a reported PKCζ inhibitor with very potent activity, which might partially explain the moderate activity of JW-1-61A. Based on the structure ...


Upregulation Of Antibiotic Activity Of A Streptomyces Sp. Via Co-Cultures With Challenge Pathogens, Anne A. Sung 2016 University of Connecticut - Storrs

Upregulation Of Antibiotic Activity Of A Streptomyces Sp. Via Co-Cultures With Challenge Pathogens, Anne A. Sung

Honors Scholar Theses

Marine natural product drug discovery has begun to play an important role in the treatment of diseases. Early drug discovery from natural products came primarily from plants, but after the discovery and development of penicillin, scientists started looking at natural products from microorganisms. Numerous natural products have been discovered from members of the order Actinomycetales, particularly in the genus Streptomyces, due to their metabolic diversity in the production of biologically active secondary metabolites. Ascidians, also known as tunicates, are marine invertebrates that contain many host-associated microbes. Adult tunicates are sessile, which makes them vulnerable to predators, and thus, they are ...


Urinary Alkalisation For Symptomatic Uncomplicated Urinary Tract Infection In Women (Review), Dermot B. O'Kane, Sameer Dave, Neel Gore, Farhaan Patel, Tammy Hoffmann, Jeanne L. Trill, Chris del Mar 2016 Bond University

Urinary Alkalisation For Symptomatic Uncomplicated Urinary Tract Infection In Women (Review), Dermot B. O'Kane, Sameer Dave, Neel Gore, Farhaan Patel, Tammy Hoffmann, Jeanne L. Trill, Chris Del Mar

Christopher Del Mar

Background

Uncomplicated urinary tract infection (UTI) is the most common bacterial infection in women, characterised by dysuria and urinary frequency. Urinary alkalisers are widely used in some countries for the symptomatic treatment of uncomplicated UTI, and they are recommended in some national formularies. However, there is a lack of empirical evidence to support their use for UTI and some healthcare guidelines advise against their use.

Objectives

We aimed to look at the benefits and harms of the use of urinary alkalisers for the treatment of uncomplicated UTIs in adult women.

Search methods

We searched the Cochrane Kidney and Transplant Specialised ...


Rapid Effects Of Aldosterone And Spironolactone In The Isolated Working Rat Heart, John C. Barbato, Patrick J. Mulrow, Joseph I. Shapiro MD, Roberto Franco-Saenz 2016 Marshall University

Rapid Effects Of Aldosterone And Spironolactone In The Isolated Working Rat Heart, John C. Barbato, Patrick J. Mulrow, Joseph I. Shapiro Md, Roberto Franco-Saenz

Joseph I Shapiro MD

Chronic administration of aldosterone promotes myocardial fibrosis in rats. The Randomized Aldactone Evaluation Study reported that the aldosterone antagonist spironolactone improved outcome in patients with congestive heart failure, suggesting a deleterious effect of aldosterone in the heart. Aldosterone has been shown to have rapid nongenomic effects in different tissues including the heart. However, the hemodynamic actions of aldosterone and spironolactone are not well characterized. In this study, we examined the hemodynamic effects of aldosterone and its receptor antagonist, spironolactone, in the isolated rat heart by use of the Langendorff-Neely technique. Perfusion with 10 nmol/L aldosterone increased contractility by 45 ...


Identification Of Potential Drug Targets In Cancer Signaling Pathways Using Stochastic Logical Models, Peican Zhu, Hamidreza Montazeri Aliabadi, Hasan Uludag, Jie Han 2016 Northwestern Polytechnical University

Identification Of Potential Drug Targets In Cancer Signaling Pathways Using Stochastic Logical Models, Peican Zhu, Hamidreza Montazeri Aliabadi, Hasan Uludag, Jie Han

Pharmacy Faculty Articles and Research

The investigation of vulnerable components in a signaling pathway can contribute to development of drug therapy addressing aberrations in that pathway. Here, an original signaling pathway is derived from the published literature on breast cancer models. New stochastic logical models are then developed to analyze the vulnerability of the components in multiple signalling sub-pathways involved in this signaling cascade. The computational results are consistent with the experimental results, where the selected proteins were silenced using specific siRNAs and the viability of the cells were analyzed 72 hours after silencing. The genes elF4E and NFkB are found to have nearly no ...


Targeted Scvegf/(177)Lu Radiopharmaceutical Inhibits Growth Of Metastases And Can Be Effectively Combined With Chemotherapy, Mary Rusckowski, Yuzhen Wang, Francis G. Blankenberg, Zoia Levashova, Marina V. Backer, Joseph M. Backer 2016 University of Massachusetts Medical School

Targeted Scvegf/(177)Lu Radiopharmaceutical Inhibits Growth Of Metastases And Can Be Effectively Combined With Chemotherapy, Mary Rusckowski, Yuzhen Wang, Francis G. Blankenberg, Zoia Levashova, Marina V. Backer, Joseph M. Backer

Radiology Publications and Presentations

BACKGROUND: scVEGF/(177)Lu is a novel radiopharmaceutical targeted by recombinant single-chain (sc) derivative of vascular endothelial growth factor (VEGF) that binds to and is internalized by vascular endothelial growth factor receptors (VEGFR). scVEGF/(177)Lu potential as adjuvant and neoadjuvant anti-angiogenic therapy was assessed in metastatic and orthotopic mouse models of triple-negative breast cancer.

METHODS: Metastatic lesions in Balb/c mice were established by intracardiac injection of luciferase-expressing 4T1luc mouse breast carcinoma cells. Mice with metastatic lesions received single intravenous (i.v.) injection of well-tolerated dose of scVEGF/(177)Lu (7.4 MBq/mouse) at day 8 after 4T1luc ...


Bupropion Hydrochloride, Cylie A. Couch 2016 Parkland Regional College

Bupropion Hydrochloride, Cylie A. Couch

Natural Sciences Poster Sessions

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to r bupropion hydrochloride (Wellbutrin, Zyban), a medication used to treat depression, smoking cessation, and seasonal affective disorder.


Aprepitant, Genesis N. Pagan 2016 Parkland College

Aprepitant, Genesis N. Pagan

Natural Sciences Poster Sessions

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Aprepitant, also known as Emend, a medication used to prevent acute and delayed nausea and vomiting associated with emetogenic chemotherapy.


Design And Structure-Activity Relationship Of Small Molecule C-Terminal Binding Protein (Ctbp) Inhibitors And Investigation Of The Scope Of Palladium Multi-Walled Carbon Nanotubes (Pd-Mwcnt) Catalyst In C–H Activation Reactions, Sudha Korwar 2016 Virginia Commonwealth University

Design And Structure-Activity Relationship Of Small Molecule C-Terminal Binding Protein (Ctbp) Inhibitors And Investigation Of The Scope Of Palladium Multi-Walled Carbon Nanotubes (Pd-Mwcnt) Catalyst In C–H Activation Reactions, Sudha Korwar

Theses and Dissertations

C-terminal binding proteins (CtBPs) are transcriptional co-repressors involved in developmental processes, and also implicated in a number of breast, ovarian, colon cancers, and resistance against cancer chemotherapy. CtBP is a validated novel potential anti-cancer target. In this project we sought to develop potent and selective small-molecule inhibitors of CtBP. Using a combination of classical medicinal chemistry and modern computational approaches, we designed a potent inhibitor HIPP (hydroxyimino-3-phenylpropanoic acid) that showed an IC50 of 0.24 μM against recombinant CtBP. Further elucidation of the structure-activity relationship (SAR) of HIPP led to the design of more potent inhibitors 3-Cl HIPP (CtBP ...


An Evaluation Of Antibiotic Resistance: Structure-Activity Relationship Studies Of Tetracyclic Indolines As A Novel Class Of Resistance-Modifying Agents For Mrsa & Analysis Of Recent Fda Regulations On Antibiotic Use In Livestock, Lakota K. Cleaver 2016 University of Colorado, Boulder

An Evaluation Of Antibiotic Resistance: Structure-Activity Relationship Studies Of Tetracyclic Indolines As A Novel Class Of Resistance-Modifying Agents For Mrsa & Analysis Of Recent Fda Regulations On Antibiotic Use In Livestock, Lakota K. Cleaver

Undergraduate Honors Theses

While the rate at which resistance develops against antimicrobials rises, research and development for new antimicrobials declines. By placing selective pressure on bacteria we are inadvertently forcing bacteria into expressing and propagating genes conferring high levels of resistance. Continued misuse and overuse of antibiotics, in light of the evident problem developing, must be resolved. To find a resolve, a multidisciplinary and multifaceted approach must be taken which involves 1) research and development of novel antimicrobial agents and 2) governmental regulation.

Strides in new antimicrobial drug development largely revolve around making old antibiotics usable again. Resistance-Modifying Agents (RMAs) act to re-sensitize ...


Synthesis, Characterization, And In Vitro Anti-Tumor Studies Of Bis Imidazolium Salts With Alkyl Chain Linkers And Naphthylmethyl Substituents, Steven R. Crabtree 2016 The University of Akron

Synthesis, Characterization, And In Vitro Anti-Tumor Studies Of Bis Imidazolium Salts With Alkyl Chain Linkers And Naphthylmethyl Substituents, Steven R. Crabtree

Honors Research Projects

Bis imidazolium salts, with alkyl chain linkers ranging from methylene to dodecyl, were synthesized with naphthylmethyl substituents at the N1 and N1’ positions for a structure-activity relationship (SAR) study. All compounds were characterized by 1H and 13C NMR spectroscopy. The cationic portion of 2 as the PF6 salt, 3, 4, and 5 were also characterized by single-crystal X-ray crystallography. Compounds 1-8, 10, and 12 were tested for their in vitro anti-cancer activity against four NSCLC cell lines via the MTT assay (NCI–H460, NCI–H1975, HCC827, and A549). Compounds 10 and 12 which contained the ...


The Synthesis And Applications Of [2.2]Paracyclophane Derivatives, Craig Hicks 2016 Dublin Institute of Technology

The Synthesis And Applications Of [2.2]Paracyclophane Derivatives, Craig Hicks

Doctoral

This work concerns the preparation of novel [2.2]paracyclophane derivatives intended for use as asymmetric ligands and investigations into surface coatings prepared from [2.2]paracylophanes. This begins with a general introduction to enantioselective synthesis, followed by a review of relevant reported ligands based on the [2.2]paracyclophane framework and their applications. Next is described the preparation of novel ligands based on the [2.2]paracyclophane structure. Starting with the preparation of a range of mono and disubstituted [2.2]paracyclophanes, including several novel analogues, this moves on to investigating resolution procedures where a novel method for the ...


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