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Articles 1 - 14 of 14
Full-Text Articles in Pharmacy and Pharmaceutical Sciences
Cyclin E Induction And Oncolytic Replication Of E1b-Deleted Adenoviruses., Pei-Hsin Cheng
Cyclin E Induction And Oncolytic Replication Of E1b-Deleted Adenoviruses., Pei-Hsin Cheng
Electronic Theses and Dissertations
Virus-mediated oncolysis has been considered as a new and promising cancer therapeutic approach. Although adenoviruses (Ads) with deletion of E1b55K preferentially replicate in cancer cells and have been used in numerous cancer treatments, the selective replication mechanism of this kind of virus still remains controversial. The lack of a well-established studies focusing on possible mechanisms enabling tumor selectivity of oncolytic Ads has hindered the further development of virotherapies and limits their clinical applications. Therefore, uncovering the molecular basis behind the tumor-killing phenomena will fill critical gaps in our understanding of the oncolytic adenovirology. Previously our laboratory has demonstrated that Ad …
Role Of Ethanol As A Cofactor In Haart Induced Hepatic Steatosis And Injury., Hridgandh Donde
Role Of Ethanol As A Cofactor In Haart Induced Hepatic Steatosis And Injury., Hridgandh Donde
Electronic Theses and Dissertations
Highly Active Antiretroviral Therapy (HAART) has led to a significant increase in the life expectancy of HIV patients; however, there are significant side effects including lipodystrophy and hepatotoxicity. Alcohol abuse is highly prevalent in HIV infected individuals and hence may be a significant negative cofactor in HAART induced hepatotoxicity. The present study examines the mechanisms underlying HAART and alcohol induced hepatotoxicity. The effects of HAART drugs (azidothymidine, and Indinavir sulphate) in combination with alcohol were examined in in vivo animal model. Alcohol and HAART drug interactions and hepatotoxicity were also assessed in-vivo using an animal model of chronic alcohol feeding. …
Metabolic Stability And Pharmacokinetics In Lead Optimization Of Potential Anti-Psychostimulant Pharmacotherapies, Seshulatha Jamalapuram
Metabolic Stability And Pharmacokinetics In Lead Optimization Of Potential Anti-Psychostimulant Pharmacotherapies, Seshulatha Jamalapuram
Electronic Theses and Dissertations
Drug addiction is a chronic disorder characterized by obsessive and uncontrollable drug-seeking behaviors. It is a major public health problem globally as well as in the United States. Apart from causing severe medical complications it also leads to several socioeconomic problems like healthcare expenditures, lost earnings and increase in drug-related crime. The discovery and development of potential pharmacotherapies to treat cocaine dependence has been a high priority for more than two decades but still there is US-FDA approved medication. This illustrates the need for the development of effective medication to treat cocaine and methamphetamine abuse. Sigma receptors have recently been …
Dual Targeting Ligands Of Sigma Receptors And Dopamine Transporters As Potential Pharmacotherapy For Cocaine Abuse, Shivangi Awasthi
Dual Targeting Ligands Of Sigma Receptors And Dopamine Transporters As Potential Pharmacotherapy For Cocaine Abuse, Shivangi Awasthi
Electronic Theses and Dissertations
No abstract provided.
Part A: Antimalarial Agents Modified At The C-16 Position Of Artemisinin; Part B: Lead Optimization Of Falcipain-2 And Falcipain-3 Inhibitors, Yunshan Wu
Electronic Theses and Dissertations
Part A: Antimalarial Agents modified at the C-16 position of Artemisinin. Malaria is a widespread tropical and subtropical parasitic disease which is caused by malarial parasites and transmitted by the infected anopheles mosquitoe. The natural product artemisinin and its derivatives are currently considered the most effective drugs against drug resistant plasmodium falciparum. However, its undesired physicochemical proprieties have limited its usage. In order to improve its effectiveness, scientists around the world have developed novel methodology to synthesize artemisinin derivatives on different positions of the artemisinin skeleton. Previous work in our group has shown that many analogues modified at the C-16 …
Molecular Modeling And Sar Studies Of Cdk5/P25 Selective Inhibitors, Arindam Chatterjee
Molecular Modeling And Sar Studies Of Cdk5/P25 Selective Inhibitors, Arindam Chatterjee
Electronic Theses and Dissertations
Alzheimer's disease (AD) is one of the most dreaded forms of progressive neurodegenerative diseases. The two main hallmarks of AD are the formation of amyloid senile plaques and neurofibrillary tangles. Cyclin dependent kinase 5 (CDK5) is a proline directed serine/threonine kinase, which expressed primarily in the central nervous system. In the biochemical process the CDK5-natural activator, p35 is cleaved by calpain to a shorter protein p25, which in turn hyperphosphorylates Tau, forms neurofibrillary tangles and causes AD. CDK5 deregulation is also indicated in other neurodegenerative diseases, such as Huntington's chorea, stroke, Parkinson's disease, amyotrophic lateral sclerosis, major depression and substance …
The Design, Synthesis, And Biological Evaluation Of Aplysinopsin Analogs As Potential Neuromodulators, Kevin Lewellyn
The Design, Synthesis, And Biological Evaluation Of Aplysinopsin Analogs As Potential Neuromodulators, Kevin Lewellyn
Electronic Theses and Dissertations
Aplysinopsins are tryptophan-derived natural products that have been isolated from a variety of marine organisms and have been shown to possess a range of biological activities. Initial synthesis of a library of 50 aplysinopsin analogs revealed that of the 12 serotonin receptor subtypes and 34 other CNS receptors, aplysinopsin analogs shoa high affinity for the 5-HT2B and 5-HT2C receptor subtypes, with selectivity for 5-HT2B over 5-HT2C. Bromination at C-4 and C-5 of the indole ring resulted in greater binding affinities, with Ki's as low as 35 nM. In addition, biological evaluation of the MAO-A and MAO-B inhibitory activities of these …
Characterization Of Different Hydrophilic Polymers And Their Applicability In Hot Melt Extrusion Technology, Sindhuri Maddineni
Characterization Of Different Hydrophilic Polymers And Their Applicability In Hot Melt Extrusion Technology, Sindhuri Maddineni
Electronic Theses and Dissertations
Research in the pharmaceutical field involves investigation of a new drug, delivery route, a delivery system, a technology to design the delivery system, or a combination thereof. Scientists have explored several delivery routes such as oral, pulmonary, nasal, injection/implant, transdermal/dermal, transmucosal etc. for their potential to transport a variety of small and large drug molecules. In the present research work, oral route, a widely accepted route of administration, for the delivery of products with a major market share, has been considered for the delivery of poorly soluble actives. The use of appropriate carrier matrices (polymers) and excipients help in incorporating …
Community Pharmacists' Attitudes Toward An Expanded Class Of Nonprescription Drugs, Ruchitbhai Mukesh Shah
Community Pharmacists' Attitudes Toward An Expanded Class Of Nonprescription Drugs, Ruchitbhai Mukesh Shah
Electronic Theses and Dissertations
Objectives: there has been considerable discussion about creating a third class of drugs which would not require a prescription, but require a pharmacist's consultation upon purchase. Very recently the Food and Drug Administration (FDA) held a hearing which repositioned a third class as an expanded nonprescription drug class termed as the "new paradigm" using certain innovative technologies. The specific objectives of this study were to: 1) measure community pharmacists' attitudes toward an expanded nonprescription drug class under the FDA’s proposed "new paradigm"; 2) determine if attitudes of community pharmacists toward an expanded nonprescription drug class under the FDA’s proposed "new …
Structural Characterization And Bioactivity Of Cranberry Oligosaccharides, Kimberly M. Auker
Structural Characterization And Bioactivity Of Cranberry Oligosaccharides, Kimberly M. Auker
Electronic Theses and Dissertations
Complex carbohydrates from plant sources, such as the fruits of cranberry (Vaccinium macrocarpon Aiton), promote human health in a variety of ways. However, complete studies of carbohydrate function often hinge on a detailed understanding and thorough elucidation of the chemical structure. Several methods have been used in the structure elucidation of cranberry oligosaccharides, such as derivatization folloby analysis using gas chromatography-mass spectrometry (GC-MS). In this manner, the identity and quantity of glycosyl units within two cranberry oligosaccharides were investigated through hydrolysis of the oligomers and subsequent synthesis of trimethylsilyl and alditol acetate derivatives. Further analysis using partially methylated alditol acetate …
Concurrent Adherence To Multiple Chronic Disease Medications: Examining The Behavior And Issues Concerning Its Measurement, Ram Sankar Basak
Concurrent Adherence To Multiple Chronic Disease Medications: Examining The Behavior And Issues Concerning Its Measurement, Ram Sankar Basak
Electronic Theses and Dissertations
Objectives the objectives were to 1) examine adherence to multiple medications prescribed for a chronic disease (intra-disease multiple medication adherence) and that of multiple chronic diseases (inter-disease multiple medication adherence); 2) determine appropriate measurement paradigm from different intra-disease multiple medication adherence measurement approaches; 3) identify optimal cut-point for a dichotomized composite measure. Methods a retrospective study design was used. The subjects came from the marketscanâ® commercial claims and encounters data 2002-2003 and filled both sulfonylurea (su) and thiazolidinedione (tzd). Adherence was measured by proportion of days covered (pdc) over each period of 30 or 90 days and cumulatively. Random components …
Synthesis Of Natural Product-Based Sphingosine Derivatives, Zarana Daksh Chauhan
Synthesis Of Natural Product-Based Sphingosine Derivatives, Zarana Daksh Chauhan
Electronic Theses and Dissertations
Marine sponges represent an excellent source of sphingolipids and their metabolites, especially sphingosine-1-phosphate (S1P). S1P plays an important role in cell differentiation, survival, proliferation and the immune response. The enzyme sphingosine kinase (SK) is critical for the phosphorylation of sphingosine to S1P and has been examined as a druggable target for the treatment of hyper-proliferative diseases, inflammation, cancer and other pathological conditions. Natural products that consist of an azetidine ring represents an interesting class of conformationally constrained scaffolds that may serve as effective lead compounds for SK inhibitor development. Hence, the goal of this thesis research was to synthesize natural-product …
Scaffold Perception, Compharmacophore Model Development, And Quantitative Structure-Affinity Relationships Of Sigma Site Ligands, David Enos Watson
Scaffold Perception, Compharmacophore Model Development, And Quantitative Structure-Affinity Relationships Of Sigma Site Ligands, David Enos Watson
Electronic Theses and Dissertations
Sigma receptors are endogenous proteins with potential utility in treating psychological disorders, ischemia, the psychological and convulsive effects of drugs of abuse, and as an imaging agent for cancerous tissues, among others. Drug design efforts targeting these receptors have been hindered by a lack of structural information of the receptors themselves. Traditional ligand-based approaches have succeeded in generating many compounds with high affinity, and quite a few with selectivity for σ-1 receptors. There are few selective ligands for use as pharmacological probes for the σ-2 receptor. Much effort has gone into exploring the structure activity relationships of ligands targeting these …
Potential Natural Product Phosphodiesterase Inhibitors, Michael John Cunningham
Potential Natural Product Phosphodiesterase Inhibitors, Michael John Cunningham
Electronic Theses and Dissertations
Three different studies set forth to investigate the role of phosphodiesterase (PDE) enzyme inhibitors in sexual dysfunction and mood regulation. First, naturalproducts were screened by computer modeling of PDE5A1. Second, compounds were isolated from a plant traditionally used as an aphrodisiac. Third, a new synthesis of psychoactive PDE4 inhibitor was attempted. An in silico screen was performed using chemical structures of isolated compounds thought to have some PDE inhibitory activity based on traditional use of the plants. A collection of compounds with structures similar to known natural product inhibitors was also included in the docking library. Glide docking software (Schrödinger) …