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Medicinal and Pharmaceutical Chemistry Commons

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Incidence, Risk Factors, And Prediction Of Gastrointestinal And Intracranial Bleeding In A Cohort Of Older Veterans Prescribed Oral Anticoagulants, Angela Laurio 2018 City University of New York (CUNY)

Incidence, Risk Factors, And Prediction Of Gastrointestinal And Intracranial Bleeding In A Cohort Of Older Veterans Prescribed Oral Anticoagulants, Angela Laurio

Dissertations and Theses

ABSTRACT

Incidence, Risk Factors, and Prediction of Gastrointestinal and

Intracranial Bleeding in a Cohort of Older Veterans Prescribed Oral Anticoagulants

by

Angela L. Laurio

Advisor: Marianne (Mimi) C. Fahs, PhD, MPH

Objectives:

The objectives of this dissertation were to: (1) describe and compare the incidence and odds of gastrointestinal and intracranial bleeding in veterans age 50 to 89 who were prescribed warfarin, direct oral anticoagulants, or no oral anticoagulants; (2) identify risk factors for gastrointestinal and intracranial bleeding among older veterans prescribed oral anticoagulants, and to calculate the relative risk of bleeding over time through time-to-event analysis; and (3) develop ...


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 ...


Novel Determinants That Influence Azole Susceptibility In Candida Glabrata And Candida Albicans, Sarah Garland Whaley 2018 University of Tennessee Health Science Center

Novel Determinants That Influence Azole Susceptibility In Candida Glabrata And Candida Albicans, Sarah Garland Whaley

Theses and Dissertations (ETD)

Despite the scientific and medical communities’ best efforts, the incidence of fungal infections in susceptible populations continues to rise. The most common cause of these opportunistic fungal infections is Candida. In fact, Candida is the fourth most common pathogen associated with nosocomial blood stream infections. Reported mortality rates for patients with candidemia vary, but have not decreased in the past fifteen years and are reported to be as high as 50%. Candida glabrata, second only to Candida albicans among Candida infections, expresses high rates of resistance to treatment with arguably the best class of currently available antifungals - the azoles.

Other ...


Synthesis And Cytotoxicity Of Azaheterocyclic Compounds, Keyur M. Pandya 2018 Rowan University

Synthesis And Cytotoxicity Of Azaheterocyclic Compounds, Keyur M. Pandya

Theses and Dissertations

Multicomponent coupling reactions (MCRs) have been known for a long time and one such reaction that utilizes isocyanides is Passerini reaction. It is a powerful tool to synthesize libraries of different compounds. Azaheterocyclic compounds play an important role in medicinal chemistry. Motifs such as imidazoles, piperazines, pyrazoles, pyridines, triazoles, etc. are routinely observed in several compounds of pharmacological interest. Several natural products also contain these motifs in them. We have undertaken a library synthesis of heterocyclic molecules driven by our group's long-standing interest of synthesizing medicinally relevant small molecules employing green chemistry techniques.

This thesis details our efforts on ...


Linear Ubiquitin Chain-Binding Domains, Lilian Fennell, Simin Rahighi, Fumiyo Ikeda 2018 Vienna BioCenter

Linear Ubiquitin Chain-Binding Domains, Lilian Fennell, Simin Rahighi, Fumiyo Ikeda

Pharmacy Faculty Articles and Research

Ubiquitin modification (ubiquitination) of target proteins can vary with respect to chain lengths, linkage type, and chain forms, such as homologous, mixed, and branched ubiquitin chains. Thus, ubiquitination can generate multiple unique surfaces on a target protein substrate. Ubiquitin‐binding domains (UBDs) recognize ubiquitinated substrates, by specifically binding to these unique surfaces, modulate the formation of cellular signaling complexes and regulate downstream signaling cascades. Among the eight different homotypic chain types, Met1‐linked (also termed linear) chains are the only chains in which linkage occurs on a non‐Lys residue of ubiquitin. Linear ubiquitin chains have been implicated in immune ...


A Study Of Albendazole And Artemisinin Drugs Under Electrochemical Oxidation, Zahilis A. Mazzochette 2018 Rowan University

A Study Of Albendazole And Artemisinin Drugs Under Electrochemical Oxidation, Zahilis A. Mazzochette

Theses and Dissertations

This work is aimed to investigate the metabolic behavior of albendazole and artemisinin. The electrochemical oxidation and reduction of these drugs were performed on electrode materials to mimic their metabolism in vivo using cyclic voltammetry and bulk electrolysis analysis. The oxidation of albendazole on gold electrode surface yielded albendazole sulfoxide and albendazole sulfone which are the main metabolites of this drug in vivo. Reduction of artemisinin on glassy carbon (GC) electrode surface yielded dihydroartemisinin and deoxy artemisinin. The formation of these products was monitored using liquid chromatography and mass spectrometry techniques. The redox processes for both drugs were shown to ...


Comparing The Side Effects Of Prescription Opioids And Medicinal Marijuana In The Treatment Of Chronic Pain, Callie Glenn, Ryan Bopp 2018 Carroll College - Helena

Comparing The Side Effects Of Prescription Opioids And Medicinal Marijuana In The Treatment Of Chronic Pain, Callie Glenn, Ryan Bopp

Carroll College Student Undergraduate Research Festival

Opioids are medications that interact with receptors in the central nervous system to provide pain relief, and have been a standard foundation for treatment of chronic pain since their discovery. But advancements in medical technology have led to the discovery of several alternatives to narcotics, one being medical marijuana. Cannabis has become increasingly pertinent in the medical field due to the medicinal and recreational legalization of the substance in several states. The purpose of this Evidence Based Practice Brief is to determine how the side effects of medical marijuana compared to those of opioid treatment affect quality of life for ...


Refrigerated Stability Of Diluted Cisatracurium, Rocuronium, And Vecuronium For Skin Testing After Perioperative Anaphylaxis, Kristen Dinsmore, Bethany Campbell, Timothy Archibald, Greg Mosier, Stacy Brown PhD, Alexei Gonzalez-Estrada MD 2018 East Tennessee State University

Refrigerated Stability Of Diluted Cisatracurium, Rocuronium, And Vecuronium For Skin Testing After Perioperative Anaphylaxis, Kristen Dinsmore, Bethany Campbell, Timothy Archibald, Greg Mosier, Stacy Brown Phd, Alexei Gonzalez-Estrada Md

Appalachian Student Research Forum

Rationale: The purpose of this study is to investigate the stored stability of dilutions of neuromuscular blocking agents (NMBAs), namely cisatracurium, rocuronium, and vecuronium, for skin prick/intradermal testing.

Methods: Concentrations of NMBAs were monitored by liquid chromatography-mass spectrometry (LC-MS/MS) for a period of 14 days. Dilutions of NMBAs were prepared in saline by factors of 10x, 100x, 1,000x, 10,000x, and 100,000x as sensitivity of the assay allowed. Diluted drug products were stored in a laboratory refrigerator until sampling. On sampling days, aliquots of each dilution were removed and compared to a freshly prepared set of ...


Investigation Of New Metal-Binding Groups For Histone Deacetylase Inhibitors, Jade McDaniel, L. M. Viranga Tillekeratne Dr. 2018 The University of Toledo

Investigation Of New Metal-Binding Groups For Histone Deacetylase Inhibitors, Jade Mcdaniel, L. M. Viranga Tillekeratne Dr.

Scholars' Celebration: Undergraduate Research Showcase

Each year, millions of people are diagnosed with cancer. In order to fight back, countless drugs are currently being developed as possible treatments for the disease. Histone deacetylase (HDAC) inhibitors are chemical compounds that can be used to reverse repressed transcription of tumor suppressor genes. They are currently used to treat several targeted cancers, but there is much room for improvement to make them work more efficiently without causing unwanted side effects. The aim of our research was to investigate new metal-binding groups to be incorporated into HDAC inhibitors and make them more class or isoform selective. In order to ...


Novel Aminobenzoboroxoles As Potential Anti-Cancer Agents, Bhawankumar Pravinchandra Patel 2018 Rowan University

Novel Aminobenzoboroxoles As Potential Anti-Cancer Agents, Bhawankumar Pravinchandra Patel

Theses and Dissertations

Boronic acids are a promising class of compounds due to their wide range of applications in medicinal and materials chemistry, and as coupling agents in organic synthesis. B-hydroxy-1,2-oxaborolanes (benzoboroxoles) are categorized as cyclic boronic acid derivatives and they are very important organic molecules because of their metabolic stability and their ability to undergo important C-C bond forming reactions such as Suzuki cross coupling. Several of these cyclic boronic acids are found to have promising pharmacological properties as antifungal, antimalarial and anti-inflammatory agents. However, based on the literature reports, synthesis of highly functionalized benzoboroxoles is typically cumbersome and not very ...


Cost-Effectiveness Analysis Of Metformin+Dipeptidyl Peptidase-4 Inhibitors Compared To Metformin+Sulfonylureas For Treatment Of Type 2 Diabetes, Christina S. Kwon, Enrique Seoane-Vazquez, Rosa Rodriguez-Monguio 2018 MCPHS University

Cost-Effectiveness Analysis Of Metformin+Dipeptidyl Peptidase-4 Inhibitors Compared To Metformin+Sulfonylureas For Treatment Of Type 2 Diabetes, Christina S. Kwon, Enrique Seoane-Vazquez, Rosa Rodriguez-Monguio

Pharmacy Faculty Articles and Research

Background: Patients with type 2 diabetes (T2D) typically use several drug treatments during their lifetime. There is a debate about the best second-line therapy after metformin monotherapy failure due to the increasing number of available antidiabetic drugs and the lack of comparative clinical trials of secondary treatment regimens. While prior research compared the cost-effectiveness of two alternative drugs, the literature assessing T2D treatment pathways is scarce. The purpose of this study was to evaluate the long-term cost-effectiveness of dipeptidyl peptidase-4 inhibitors (DPP-4i) compared to sulfonylureas (SU) as second-line therapy in combination with metformin in patients with T2D.

Methods: A Markov ...


The Development Of Novel Non-Peptide Proteasome Inhibitors For The Treatment Of Solid Tumors, Zachary C. Miller 2018 University of Kentucky

The Development Of Novel Non-Peptide Proteasome Inhibitors For The Treatment Of Solid Tumors, Zachary C. Miller

Theses and Dissertations--Pharmacy

The proteasome is a large protein complex which is responsible for the majority of protein degradation in eukaryotes. Following FDA approval of the first proteasome inhibitor bortezomib for the treatment of multiple myeloma (MM) in 2003, there has been an increasing awareness of the significant therapeutic potential of proteasome inhibitors in the treatment of cancer. As of 2017, three proteasome inhibitors are approved for the treatment of MM but in clinical trials with patients bearing solid tumors these existing proteasome inhibitors have demonstrated poor results. Notably, all three FDA-approved proteasome inhibitors rely on the combination a peptide backbone and reactive ...


Pde8 Is Expressed In Human Airway Smooth Muscle And Selectively Regulates Camp Signaling By Β 2 Ar-Ac6, Timothy B. Johnstone, Kaitlyn H. Smith, Cynthia J. Koziol-White, Fengying Li, Austin G. Kazarian, Maia L. Corpuz, Maya Shumyachter, Frederick J. Ehlert, Bianca E. Himes, Reynold A. Pannettieri Jr., Rennolds S. Ostrom 2017 Chapman University

Pde8 Is Expressed In Human Airway Smooth Muscle And Selectively Regulates Camp Signaling By Β 2 Ar-Ac6, Timothy B. Johnstone, Kaitlyn H. Smith, Cynthia J. Koziol-White, Fengying Li, Austin G. Kazarian, Maia L. Corpuz, Maya Shumyachter, Frederick J. Ehlert, Bianca E. Himes, Reynold A. Pannettieri Jr., Rennolds S. Ostrom

Pharmacy Faculty Articles and Research

Two cAMP signaling compartments centering around adenylyl cyclase (AC) exist in human airway smooth muscle (HASM) cells, one containing ß2AR-AC6 and another containing E prostanoid receptors (EPR)-AC2. We hypothesized that different phosphodiesterase (PDE) isozymes selectively regulate cAMP signaling in each compartment. According to RNA-seq data, 18 of 24 PDE genes were expressed in primary HASM cells derived from age- and gender-matched donors with and without asthma. PDE8A was the third most abundant of the cAMP-degrading PDE genes, after PDE4A and PDE1A. Knockdown of PDE8A using shRNA evoked 2-fold greater cAMP responses to 1 DM forskolin in the presence of ...


Green Chemistry Oxidative Modification Of Peptoids Utilizing Bleach And Tempo, Jesse Leland Roberts 2017 University of Arkansas, Fayetteville

Green Chemistry Oxidative Modification Of Peptoids Utilizing Bleach And Tempo, Jesse Leland Roberts

Theses and Dissertations

Biotherapeutic drugs, derived from biological molecules such as proteins and DNA, are becoming an integral and exceptionally critical aspect of modern medicine. Compared to common pharmaceutical drugs, biotherapeutics are much larger in size and have greater target specificity, allowing them to treat many chronic diseases ranging from cancer to rheumatoid arthritis. The major issue with protein based therapeutics is that they readily undergo proteolysis, or enzymatic degradation, when administered through subcutaneous injections. Traditionally, biotherapeutic modification procedures have centered on the use of PEG derivatives. This process, called PEGylation, is unfavorable due to the increases in molecular weights of the proteins ...


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 ...


Diverse Amide Analogs Of Sulindac For Cancer Treatment And Prevention, Bini Mathew, Judith V. Hobrath, Michele C. Connelly, Rodney K. Guy, Robert C. Reynolds 2017 Southern Research Institute

Diverse Amide Analogs Of Sulindac For Cancer Treatment And Prevention, Bini Mathew, Judith V. Hobrath, Michele C. Connelly, Rodney K. Guy, Robert C. Reynolds

Pharmaceutical Sciences Faculty Publications

Sulindac is a non-steroidal anti-inflammatory drug (NSAID) that has shown significant anticancer activity. Sulindac sulfide amide (1) possessing greatly reduced COX-related inhibition relative to sulindac displayed in vivoantitumor activity that was comparable to sulindac in a human colon tumorxenograft model. Inspired by these observations, a panel of diverse sulindac amide derivatives have been synthesized and their activity probed against three cancer cell lines (prostate, colon and breast). A neutral analog, compound 79 was identified with comparable potency relative to lead 1 and activity against a panel of lymphoblastic leukemia cell lines. Several new series also show good activity relative ...


Role Of Microglial Amylin Receptors In Mediating Beta Amyloid (Aβ)-Induced Inflammation, Wen Fu, Vlatka Vukojevic, Aarti Patel, Rania Soudy, David MacTavish, David Westaway, Kamaljit Kaur, Valeri Goncharuk, Jack Jhamandas 2017 University of Alberta

Role Of Microglial Amylin Receptors In Mediating Beta Amyloid (Aβ)-Induced Inflammation, Wen Fu, Vlatka Vukojevic, Aarti Patel, Rania Soudy, David Mactavish, David Westaway, Kamaljit Kaur, Valeri Goncharuk, Jack Jhamandas

Pharmacy Faculty Articles and Research

Background: Neuroinflammation in the brain consequent to activation of microglia is viewed as an important component of Alzheimer’s disease (AD) pathology. Amyloid beta (Aβ) protein is known to activate microglia and unleash an inflammatory cascade that eventually results in neuronal dysfunction and death. In this study, we sought to identify the presence of amylin receptors on human fetal and murine microglia and determine whether Aβ activation of the inflammasome complex and subsequent release of cytokines is mediated through these receptors.

Methods: The presence of dimeric components of the amylin receptor (calcitonin receptor and receptor activity modifying protein 3) were ...


Development And Validation Of Triticum Phytobiological Method As An Alternative Procedure For Investigating In Vivo Acute Toxicity On Mice, Emil Ştefănescu, Aurelia N. Cristea, Cornel Chiriță, Octavian Olaru, Adriana Anghel, Mihaela Dinu 2017 Carol Davila University, Department of Pharmacology and Clinical Pharmacy, Bucharest, Romania

Development And Validation Of Triticum Phytobiological Method As An Alternative Procedure For Investigating In Vivo Acute Toxicity On Mice, Emil Ştefănescu, Aurelia N. Cristea, Cornel Chiriță, Octavian Olaru, Adriana Anghel, Mihaela Dinu

Journal of Mind and Medical Sciences

The goal of this study was to validate an alternative method for determining in vivo acute toxicity using vegetal material instead of laboratory animals, starting from the phytobiological method known also as the Triticum technique. We set out to demonstrate that vegetal cells have similar sensitivity to some toxic agents as animal cells, in which case a statistical correlation could be established. A series of new compounds synthesized by the Romanian National Institute for Chemical Pharmaceutical Research and Development as potential β3 adrenergic receptors agonists were tested for their acute toxicity using classic animal exposure models, before investigating possible anti-diabetic ...


Experimental Pharmacological Research Regarding Some Newly Synthesized Benzamides On Central Nervous System Functions, Cornel Chiriță, Emil Ștefănescu, Cristina D. Marineci, Simona Negreș, Diana C. Nuță 2017 Carol Davila University, Department of Pharmacology and Clinical Pharmacy, Bucharest, Romania

Experimental Pharmacological Research Regarding Some Newly Synthesized Benzamides On Central Nervous System Functions, Cornel Chiriță, Emil Ștefănescu, Cristina D. Marineci, Simona Negreș, Diana C. Nuță

Journal of Mind and Medical Sciences

Three newly synthesized benzamides by the Department of Pharmaceutical Chemistry of the Faculty of pharmacy from the University of Medicine and Pharmacy „Carol Davila” Bucharest were tested in order to determine whether these new molecules have similar effects on the central nervous system as those already in therapeutic use belonging to the same chemical group, such as tiapride (neuroleptic) or lidocaine (local anaesthetic). Tests were carried out on NMRI mice which were given new compounds, conventionally named I5C, I14C, and II5C in a dose of 1/20 of the lethal dose 50% (LD50), as previously determined. They received this treatment ...


Trkb-Enhancer Facilitates Functional Recovery After Traumatic Brain Injury, John Marshall, Joanna Szmydynger-Chodobska, Mengia S. Rioult-Pedotti, Kara Lau, Andrea T. Chin, Siva K. Reddy Kotla, Rakesh Tiwari, Keykavous Parang, Steven W. Threlkeld, Adam Chodobski 2017 Brown University

Trkb-Enhancer Facilitates Functional Recovery After Traumatic Brain Injury, John Marshall, Joanna Szmydynger-Chodobska, Mengia S. Rioult-Pedotti, Kara Lau, Andrea T. Chin, Siva K. Reddy Kotla, Rakesh Tiwari, Keykavous Parang, Steven W. Threlkeld, Adam Chodobski

Pharmacy Faculty Articles and Research

Brain-derived neurotrophic factor (BDNF), a key player in regulating synaptic strength and learning, is dysregulated following traumatic brain injury (TBI), suggesting that stimulation of BDNF signaling pathways may facilitate functional recovery. This study investigates whether CN2097, a peptidomimetic ligand which targets the synaptic scaffold protein, postsynaptic density protein 95, to enhance downstream signaling of tropomyosin-related kinase B, a receptor for BDNF, can improve neurological function after TBI. Moderate to severe TBI elicits neuroinflammation and c-Jun-N-terminal kinase (JNK) activation, which is associated with memory deficits. Here we demonstrate that CN2097 significantly reduces the post-traumatic synthesis of proinflammatory mediators and inhibits the ...


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