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Articles 271 - 300 of 318
Full-Text Articles in Pharmacy and Pharmaceutical Sciences
Discovery Of Novel Glycogen Synthase Kinase-3beta Inhibitors: Molecular Modeling, Virtual Screening, And Biological Evaluation, Gang Fu
Electronic Theses and Dissertations
Glycogen synthase kinase-3 (GSK-3) is a multifunctional serine/threonine protein kinase which is engaged in a variety of signaling pathways, regulating a wide range of cellular processes. Due to its distinct regulation mechanism and unique substrate specificity in the molecular pathogenesis of human diseases, GSK-3 is one of the most attractive therapeutic targets for the unmet treatment of pathologies, including type-II diabetes, cancers, inflammation, and neurodegenerative disease. Recent advances in drug discovery targeting GSK-3 involved extensive computational modeling techniques. Both ligand/structure-based approaches have been well explored to design ATP-competitive inhibitors. Molecular modeling plus dynamics simulations can provide insight into the protein-substrate …
Geographic And Host-Microbe Symbiotic Influence On Secondary Metabolism, Samuel Hamed Abbas
Geographic And Host-Microbe Symbiotic Influence On Secondary Metabolism, Samuel Hamed Abbas
Electronic Theses and Dissertations
This thesis is composed of studies that regard the advancement to the Arctic region and the importance of host-microbe interactions in natural product discovery. Bioactive metabolites have been reported from a myriad of marine and terrestrial organisms around the world including plants, insects, sponges, tunicates, bacteria, and fungi among others. Many macroorganisms, of which the metabolites are found, depend on the symbiotic relationship of microorganisms for metabolite production. The scope of this work is to investigate secondary metabolism of both marine and terrestrial organisms from different areas of the world as well as search for the importance of host-microbe symbiosis …
Development And Comparative Predictive Validity Of An Outpatient Medication Exposure Measure For Risk Adjustment Using Retrospective Claims Data, Kyle Dennis Null
Development And Comparative Predictive Validity Of An Outpatient Medication Exposure Measure For Risk Adjustment Using Retrospective Claims Data, Kyle Dennis Null
Electronic Theses and Dissertations
The purpose of this study was to develop and test a measure of outpatient prescription utilization (medication exposure measure, or MEM) that may be coupled with the CMS-HCC and CMS-RxHCC methodologies to improve risk-adjusted payments to Medicare Part C and Part D plans. Studies have identified prescription measures that predict future expenditures; however, many are easily manipulable by health plans or practitioners, thus limiting their utility as risk-adjusters. The addition of a non-manipulable prescription utilization measure to existing risk-adjustment models may improve prediction, reducing adverse risk selection incentives by health plans. A secondary objective of this study was to evaluate …
The Potential For Screening For Interpersonal Violence In Community Pharmacies: An Exploratory Study, Marie Barnard
The Potential For Screening For Interpersonal Violence In Community Pharmacies: An Exploratory Study, Marie Barnard
Electronic Theses and Dissertations
Intimate partner violence (IPV) is a public health problem of epidemic proportion; the only known effective health care intervention is routine screening for IPV exposure. Despite professional guidelines for routine screening, this intervention has been poorly adopted. Expansion of screening efforts to the community pharmacy setting provides an opportunity to have a substantial impact on the health, well-being of pharmacy patients. This investigation is the first to examine IPV screening related to the pharmacy environment. An existing measure of physicians' readiness to manage IPV (PREMIS) was adapted for the community pharmacy environment and validated in a national random sample of …
Preformulation Characterization And Formulation Development Of Δ9-Tetrahydrocannabinol Prodrugs For Potential Treatment Of Glacuoma, Tushar Hingorani
Preformulation Characterization And Formulation Development Of Δ9-Tetrahydrocannabinol Prodrugs For Potential Treatment Of Glacuoma, Tushar Hingorani
Electronic Theses and Dissertations
Relationship between smoking marihuana and a drop in intraocular pressure (IOP) was first reported in 1971. Research efforts since then have identified a number of constituents that could be linked to this observation. Delta-9-Tetrahydrocannabinol (THC) was one of the ingredients identified. However, four decades and numerous research efforts since the first observation, it has still not been concluded whether THC is effective in the treatment of glaucoma or not. Current therapy for IOP control in glaucoma, though effective, cannot prevent vision loss completely. Thus, identification of agents that can lower IOP as well as protect the retinal ganglion cells from …
Design And Development Of Drug Delivery Systems For Immediate And Sustained Release Utilizing Hot Melt Extrusion, Abhilasha Singh
Design And Development Of Drug Delivery Systems For Immediate And Sustained Release Utilizing Hot Melt Extrusion, Abhilasha Singh
Electronic Theses and Dissertations
Polymers have indispensable role in pharmaceutical formulation development. Polymer choice is a critical factor to obtain the desired drug-release profile during formulation development for HME (Hot melt extrusion). Many commercially available, pharmaceutical-grade polymers can be used in HME formulations. The suitable polymer choice facilitates processing in the extruder. When choosing a polymer to use in a formulation, processing conditions and processing attributes of the active pharmaceutical ingredients (APIs) should be considered. The physicochemical and the mechanisms of drug release from drug delivery systems prepared by utilizing HME with various polymeric carriers were investigated. Amorphous forms of API can have as …
Anticancer And Antibiotic Leads From Marine Organis, Bin Wang
Anticancer And Antibiotic Leads From Marine Organis, Bin Wang
Electronic Theses and Dissertations
During the past three decades, the development of marine natural products as drug leads has become a promising avenue for research. As our efforts towards the discovery of anticancer and antibiotic drug leads from marine organisms, modifications of anticancer drug candidate kahalalide F, isolations of new peptides from the mollusk, Elysia rufescens and anticancer drug leads from the NCI repository, as well as chemical regulation of antibiotic production from marine Pseudomonas aeruginosa were investigated. Kahalalide F (KF) is a potent anticancer lead isolated from the herbivorous marine mollusk E. rufescens and its algal diet Bryopsis pennata. Our semisynthesis approach was …
Antimalarials From Plant Pathogenic Fungi, Mallika Kumarihamy
Antimalarials From Plant Pathogenic Fungi, Mallika Kumarihamy
Electronic Theses and Dissertations
The purpose of this study was to discover antimalarial compounds from necrotropic plant pathogenic fungi. Various phytotoxins released by necrotropic plant pathogenic fungi may inhibit the plant-like metabolic pathways in the apicoplast, a chloroplast-like organelle, essential for the survival of apicomplexan parasites, such as Plasmodium which cause malaria in humans. This dissertation describes the isolation, characterization, and biological evaluation of secondary metabolites of eight fungal strains. In addition to the antiplasmodial assay, all the extracts were subjected to phytotoxic, antimicrobial, and cytotoxic bioassays. Isolation of metabolites was performed by chromatographic methods and identification was carried out by spectroscopic and spectrometric …
Design And Synthesis Of Hiv-1 Integrase Inhibitors, Sarah Chajkowski Scarry
Design And Synthesis Of Hiv-1 Integrase Inhibitors, Sarah Chajkowski Scarry
Electronic Theses and Dissertations
In recent years, HIV-1 integrase (IN) has emerged as an attractive target for the treatment of human immunodeficiency virus type 1 (HIV-1), the causative pathogen of acquired immuno-deficiency syndrome (AIDS). Several classes of IN inhibitors are known but many of these compounds are toxic, do not show antiviral activity or display decreased potency. Therefore, new classes of potent IN inhibitors are desperately needed. The b-diketo (b-DK) class of compounds has emerged as one of the most successful classes of IN inhibitors. Although several b-DK inhibitors with potent antiviral activity are known, compounds containing b-DK motifs have limitations in drug development. …
Design Synthesis And Biological Evaluation Of Non-Peptide Neuropeptide Ff Ligands, Jessica Valentinas Mankus
Design Synthesis And Biological Evaluation Of Non-Peptide Neuropeptide Ff Ligands, Jessica Valentinas Mankus
Electronic Theses and Dissertations
Neuropeptide FF is an endogenous RF-amide with two receptor subtypes originally described as having anti-opioid characteristics. While peptide work helped to elucidate key features for targeting the subtypes of the neuropeptide FF receptor, non-peptide small molecules offer a more refined tool to discover features that affect selectivity and affinity. Improvements in small molecule ligands for neuropeptide FF support lead development and offer a clearer understanding of the binding pocket of each receptor subtype. Previous work on the lead 4–anilindopiperidine structure clarified a key feature between agonist and antagonist behavior. Early modifications of substituents of the piperidine nitrogen were tolerated and …
Discovery, Isolation, And Identification Of Antimalarials From Fungal Endophytes, Andrekeus Lee
Discovery, Isolation, And Identification Of Antimalarials From Fungal Endophytes, Andrekeus Lee
Electronic Theses and Dissertations
We examined fungal endophytes for their ability to inhibit bacterial, fungal and protozoal pathogens. Once antimalarial activity was discovered and confirmed, we sought to isolate and identify the active constituent(s) of our extracts. Bioassay-guided fractionation techniques were used to isolate our active compound, the structure of which was elucidated using 1H- and 13C-NMR. 2D-NMR and LC-MS analyses helped confirm that our endophytes were indeed producing artemisinin. Growth versus production studies were conducted to optimize our growth and extraction conditions while several other variables, like temperature and culture medium, were evaluated in an effort to improve our yields. Artemisinin production under …
Discovery Of Small-Molecule Natural Products That Target Cellular Bioenergetics, Sandipan Datta
Discovery Of Small-Molecule Natural Products That Target Cellular Bioenergetics, Sandipan Datta
Electronic Theses and Dissertations
Molecular-targeted antitumor therapy has found favor in antitumor drug discovery programs. Hypoxia (< 5% oxygen) is a comfeature of solid tumors and hypoxia-inducible factor-1 (HIF-1) represents an important antitumor target. Bioenergetic homeostasis is typically altered in tumor cells and HIF-1 plays an important role to produce a glycolytic phenotype. Glycolysis inhibitors are an emerging class of potential tumor-selective adjuvant therapeutic agents. Natural product aerobic glycolysis inhibitors may enhance the effectiveness of current therapies. Mitochondrial oxidative phosphorylation inhibitors in botanical dietary supplements (BDS) possess a potential health hazard which should be identified and appropriately regulated. Chapter one briefly reviews the molecular-targeted natural product antitumor drug discovery process. Descriptions of tumor hypoxia, HIF-1, HIF-1 regulatory pathways and the effect of HIF-1 on tumor cell bioenergetics are presented. Cellular bioenergetic pathways and natural products that inhibit HIF-1 by interfering with cellular bioenergetics are discussed. Mitochondriotoxic small-molecule natural products reported previously are further reviewed. Chapter two discusses the effect of chromatographic media on molecular-targeted antitumor drug discovery. A panel of crude extracts was eluted through columns of various chromatographic media using a step gradient method. Total recoveries from the various columns and various elution protocols were compared and statistically analyzed. The crude extracts and column eluates were evaluated for HIF-1 inhibitory activity. Chapter three discusses the development of a bioenergetics-based screening method to screen crude extracts for glycolysis inhibitors. Crude extracts (10,648) were screened and seven hits (hit rate 0.72%) were identified. Bioassay-guided isolation of Moronobea coccinea crude extract resulted in isolation of a protonophoric compound moronone (1) (false positive). The structure of 1 was determined by a combination of spectroscopic and spectrometric means. The protonophoric compounds must be rapidly dereplicated for successful discovery of glycolysis inhibitors. Chapter four discusses the screening of BDS products and pure compounds for mitochondrial uncouplers or electron transport chain inhibitors. The blue cohosh (Caulophyllum thalictroides) extract and three saponins cauloside A (3), saponin PE (4) and cauloside C (5) permeabilize the mitochondrial membrane. Sesamin (6) and guggulsterol III (7) and guggul (Commiphora wightii) extract inhibit mitochondrial complex I. These extracts and compounds are cytotoxic in nature.
Development Of Novel Thermosensitive Polymers For Bioresponsive Drug Delivery, Vivek Kumar Garripelli
Development Of Novel Thermosensitive Polymers For Bioresponsive Drug Delivery, Vivek Kumar Garripelli
Electronic Theses and Dissertations
Stimuli-responsive polymers have already shotremendous promise in controlled and self-regulated drug delivery. Successful construction of responsive polymers requires amalgamation of chemical, physical and biological principles. For careful therapy, a great deal of advantages offered by stimuli-responsive polymers is essential. A small or modest change in the environmental condition (e.g. temperature, pH, light) brings a sharp change in the properties of the responsive polymers. 'Smart' drug delivery systems utilize these principles to mimic the biological response behavior to a certain extent. Synthetic polymers incorporated with stimuli-responsive behavior would be amenable to overcome some of the systemic and intracellular delivery barriers. Development …
Metabolism And Pharmacokinetics In The Development Of New Therapeutics For Cocaine And Opioid Abuse, Pradeep Kumar Vuppala
Metabolism And Pharmacokinetics In The Development Of New Therapeutics For Cocaine And Opioid Abuse, Pradeep Kumar Vuppala
Electronic Theses and Dissertations
Cocaine and opioid abuse are a major public health concern and the cause of significant morbidity and mortality worldwide. The development of effective medication for cocaine and opioid abuse is necessary to reduce the impact of this issue upon the individual and society. The pharmacologic treatment for drug abuse has been based on one of the following strategies: agonist substitution, antagonist treatment, or symptomatic treatment. This dissertation is focused on the role of metabolism and pharmacokinetics in the development of new pharmacotherapies, CM304 (sigma-1 receptor antagonist), mitragynine and 7-hydroxymitragynine (μ-opioid receptor agonists), for the treatment of drug abuse. The affinity …
Biopharmaceutic And Pharmacokinetic Studies Of Sucrose Acetate Isobutyrate As An Excipient For Oral Drug Delivery., Martin Ray Tant
Biopharmaceutic And Pharmacokinetic Studies Of Sucrose Acetate Isobutyrate As An Excipient For Oral Drug Delivery., Martin Ray Tant
Electronic Theses and Dissertations
Sucrose acetate isobutyrate (SAIB), a randomly substituted sucrose approximating sucrose diacetate hexaisobutyrate, is produced by Eastman Chemical Company for a variety of applications. SAIB is widely used in the food industry as a weighting agent to disperse flavoring oils in primarily citrus-based soft drink beverages. Additionally, SAIB is currently being marketed by another company as a parenteral drug delivery system. The studies reported here focused on investigating SAIB as an excipient, or delivery vehicle, for use in oral delivery of several drugs, including ibuprofen, saquinavir, and clarithromycin. Dissolution experiments were conducted using both ibuprofen and caffeine, and results suggest that …
Biopharmaceutic And Pharmacokinetic Evaluation Of Hesperidin And Hesperetin For Ocular Delivery, Ramesh Srirangam
Biopharmaceutic And Pharmacokinetic Evaluation Of Hesperidin And Hesperetin For Ocular Delivery, Ramesh Srirangam
Electronic Theses and Dissertations
The bioflavonoid hesperidin and its aglycone hesperetin are promising candidates for the treatment of diabetic retinopathy and diabetic macular edema because of their pharmacological properties. The objective of this project was to characterize the biopharmaceutic and pharmacokinetic characteristics of hesperidin and hesperetin for ocular delivery, especially with respect to the distribution of these compounds to the posterior segment of the eye. Hesperidin and hesperetin were found to be water insoluble compounds. Although they demonstrated good permeability across the ocular tissues, hesperetin's permeability was found to be higher than that of hesperidin. Hesperidin demonstrated symmetrical transcorneal and transretinal permeation whereas hesperetin …
Biophysical Techniques Of Transcutaneous Drug Sampling And Drug Delivery, Srinivasa Murthy Sammeta
Biophysical Techniques Of Transcutaneous Drug Sampling And Drug Delivery, Srinivasa Murthy Sammeta
Electronic Theses and Dissertations
Monitoring the time course of drug in the skin is critical for determining the frequency and dose of drug administration from safety and efficacy perspectives. Intermittent blood sampling is used as a surrogate for approximating concentration of drugs in the tissues, which leads to blood loss and discomfort to patients. A novel noninvasive technique called “Electroporation and transcutaneous sampling” (ETS) was developed for estimating the drug concentration in the skin extracellular fluid. The application of ETS technique in studying dermatokinetics of cephalexin, ciprofloxacin, and 8-methoxypsoralen was investigated. The results demonstrated the ability of ETS technique in dermatokinetic studies of drugs …
Design, Synthesis, Biological Evaluation And Metabolic Stability Studies Of Sigma Receptor Ligands, Rohit Bhat
Design, Synthesis, Biological Evaluation And Metabolic Stability Studies Of Sigma Receptor Ligands, Rohit Bhat
Electronic Theses and Dissertations
Sigma receptors represent a unique family of proteins that includes two subtypes: sigma-1 and sigma-2. Sigma-1 receptors have been implicated in the behavioral and motivational effects of psychostimulants as well as in the pathophysiology of depression and Alzheimer's disease. Sigma-2 receptors are widely expressed on many tumor cells and they are believed to play an important role in tumor cell proliferation. Therefore, sigma receptors are attractive targets for developing pharmaceutical agents directed to the treatment of psychostimulant abuse, cancer, Alzheimer's disease as well as diagnostic agents for cancer and brain imaging. A derivatized 2(3H)-benzothiazolone, (3-(2-(azepan-1-yl)ethyl)-6-propylbenzo[ d]thiazol-2(3H)-one) was reported to have …
Pharmacy-Level Quality Measures And The Consumer: Preferences And Attitudes, Zainab S. Shahpurwala
Pharmacy-Level Quality Measures And The Consumer: Preferences And Attitudes, Zainab S. Shahpurwala
Electronic Theses and Dissertations
Objectives. To determine the perceptions of consumers toward community pharmacy quality measures and compare their perceptions regarding their pharmacy's overall quality before and after exposure to these measures. To explore the use of evaluative criteria applied by consumers to determine their preference for information related to these measures. Methods. Focus groups were used to refine attributes and levels used in the quantitative phase of the study. An Internet-based survey was administered to a national, online, consumer panel of community pharmacy patrons using maintenance medications. Descriptive statistics, MANOVA and t-tests were used to determine and compare perceptions related to the community …
Pharmacokinetic Evaluation Of A Novel Compound, Sn79, A Putative Sigma-2 Receptor Antagonist, By Intravenous And Oral Administration In Rats, Harsha Vinnakota
Pharmacokinetic Evaluation Of A Novel Compound, Sn79, A Putative Sigma-2 Receptor Antagonist, By Intravenous And Oral Administration In Rats, Harsha Vinnakota
Electronic Theses and Dissertations
Considering the alarming rates at which substance drug abuse, especially cocaine, is increasing in today's society, there is a lot of impetus on the development of medications that can effectively help alleviate its toxicity and addiction. The affinity of cocaine to sigma receptors (sigma-1 and sigma-2) rendered the hypothesis that blocking sigma receptors could be a possible mechanism to attenuate cocaine-induced toxicity and addiction. In this view, SN79, a synthetic compound with selectivity to both sigma-1 and sigma-2 receptors garnered our attraction for its use as an antagonist. This dissertation encompasses detailed investigation of SN79 from drug discovery and development …
The Strategic Value Driver Model: A Methodology For Examining Value Drivers For A New Pharmaceutical Product In Diabetes, Sumit Verma
Electronic Theses and Dissertations
Objective. Objective The primary objective of this study was to explore a new methodological framework—Strategic Value Driver Model (SVDM), for examining value drivers for new pharmaceutical inhaled insulin in diabetes. Methods. A cross-sectional, internet-based survey was used to collect a sample of 483 Type 2 diabetic patients via national panel of diabetic patients. The sample had two subgroups—insulin-naïve (52.9%, n=255) and insulin-user (47.1%, n=227) patients. The comparative performance of insulin syringes/vials, insulin pen and inhaled insulin was captured on four product attributes (i.e., safety, convenience, clinical efficacy and cost) after asking the patients to report the importance of these attributes. …
Natural Products Chemistry Of Leads Acting On Mrsa, Hcv, Malaria, And Depression Disorders, Mohamed Ali Mohamed Ali Ibrahim
Natural Products Chemistry Of Leads Acting On Mrsa, Hcv, Malaria, And Depression Disorders, Mohamed Ali Mohamed Ali Ibrahim
Electronic Theses and Dissertations
Nature has proven to be an endless source of abundant diversity of chemical entities with varying biological activities. The World Health Organization (WHO) estimates that 80% of the world's population depends on traditional medicine for treating their everyday health problems. According to Gordon Cragg, former director of the natural products branch of the NCI, ″Nature has produced wonderfully complex molecules that no synthetic chemist could ever dream up.″ Moreover, he emphasized that over 60% of cancer therapeutics have been derived from nature whether directly through isolation or indirectly through semi-synthesis. Various examples have been reported such as extracts from Catharanthus …
Market Response To Food And Drug Administration's Safety Warnings: A Case Study Using An Interrupted Time Series Analysis Of The Medicare Database For 2006-2008, Hafiz Oko-Osi
Electronic Theses and Dissertations
Objectives: To evaluate the impact of a safety warning on the utilization rates of thiazolidinedione oral anti-diabetes medication using an interrupted time series analysis. Methods: We extracted data from a five percent national sample of Medicare Part D beneficiaries for the periods between January 2006 and December 2008. Beneficiaries with Part D claims for thiazolidinediones were classified into appropriate-use, at risk, and contraindicated groups based on certain comorbid conditions. We assessed the effects of the May 2007 FDA safety warning about an ongoing safety review of rosiglitazone's potential to increase cardiovascular risks on thiazolidinedione utilization rates using an interrupted time …
Factors That Physicians Find Encouraging And Discouraging About Electronic Prescribing: A Quantitative Study, Krutika Satish Jariwala
Factors That Physicians Find Encouraging And Discouraging About Electronic Prescribing: A Quantitative Study, Krutika Satish Jariwala
Electronic Theses and Dissertations
Research objective. While the adoption of e-prescribing is growing, the Institute of Medicine's recommendations that all prescriptions be routed electronically by 2010 certainly has not been met. Therefore, the objective of this study is to compare the factors that physicians find encouraging and discouraging about e-prescribing based on their e-prescribing adoption status. Study design. Cross-sectional, descriptive design. An Internet-based survey was sent to national convenience sample of physicians. Using e-prescribing literature, 44 items were developed concerning various factors related to the adoption of e-prescribing. Physicians rated how much the factors encouraged them or discouraged them about e-prescribing. Analysis procedures included …
Factors Affecting Community Pharmacy Owners' Attitudes Toward And Likelihood To Adopt Rxsync Service(Sm), Namita Joshi
Factors Affecting Community Pharmacy Owners' Attitudes Toward And Likelihood To Adopt Rxsync Service(Sm), Namita Joshi
Electronic Theses and Dissertations
Factors affecting community pharmacy owners' attitudes toward and likelihood to adopt RxSync ServiceSM. Objective. There is an increased recognition of the role of pharmacists in the provision of patient care services. Therefore, understanding factors that affect pharmacists' attitudes and likelihood to implement pharmacy services is warranted. The objective of this study is to examine how community pharmacy owners' entrepreneurial and demographic characteristics, perceptions of pharmacy service characteristics (perceived benefit, perceived compatibility, and perceived complexity), workload perceptions, and the number of pharmacy services they already offer, affect their attitude toward and likelihood to adopt RxSync ServiceSM, a newly developed prescription management …
Part A: Studies Towards Total Synthesis Of An Anticancer And Antifungal Natural Product, Pseudolaric Acid B; Part B: Synthesis And Biological Evaluation Of Berkeleyamide A And Its Derivatives, Swapnil Jayant Kulkarni
Part A: Studies Towards Total Synthesis Of An Anticancer And Antifungal Natural Product, Pseudolaric Acid B; Part B: Synthesis And Biological Evaluation Of Berkeleyamide A And Its Derivatives, Swapnil Jayant Kulkarni
Electronic Theses and Dissertations
Part A: Studies towards total synthesis of an antifungal and anticancer agent, Pseudolaric acid B. Marked by the uncontrolled cell proliferation, cancer is one of the deadliest diseases, accounting for about 7.0 million deaths in 2007. Cancer is second leading cause of death worldwide, according to the American Cancer Society. Cancer chemotherapy has evolved through many years of painstaking research, and as a result, today we are able to cure at least some of cancers. One of the major impediments in the development of new drugs for treating cancer is that most of the approved drugs are themselves toxic and …
Use Of Structure-And Ligand-Based Drug Design Tools For The Discovery Of Small Molecule Inhibitors Of Cysteine Proteases For The Treatment Of Malaria And Sars Infection, Falgun Shah
Electronic Theses and Dissertations
A wide array of molecular modeling tools were utilized to design and develop inhibitors against cysteine protease of P. Falciparum Malaria and Severe Acute Respiratory Syndrome (SARS). A number of potent inhibitors were developed against cysteine protease and hemoglobinase of P. falciparum , referred as Falcipains (FPs), by the structure-based virtual screening of the focused libraries enriched in soft-electrophiles containing compounds. Twenty one diverse, non-peptidic, low micromolar hits were identified. A combined data mining and combinatorial library synthesis approach was performed to discover analogs of virtual screening hits and establish the structure-activity relationships (SAR). However, the resulting SAR of the …
New Synthetic Methodologies For The Construction And Optimization Of Natural Products, Amir E. Wahba
New Synthetic Methodologies For The Construction And Optimization Of Natural Products, Amir E. Wahba
Electronic Theses and Dissertations
Toxicity associated with bioactive natural products is considered as a major obstacle in the process of drug discovery. Manzamine A (MA) is one such candidate that requires optimization to overcome the toxicity problem. The manzamine alkaloids represents a unique class of natural products that have shown a diverse range of bioactivities including antimicrobial, antiparasitic, cytotoxicity, anti-inflammatory, pesticidial, and was shown to possess activity against HIV-1 and AIDS opportunistic infections. The greatest potential for the manzamine alkaloids appears to be against malaria and neuroinflammation. Experimental and modeling studies suggested that the planer ?-carboline moiety can act as DNA intercalator and hence …
Do Statins Improve Outcomes In Patients With Asthma On Inhaled Corticosteroid Therapy? A Retrospective Analysis Of The Mississippi Medicaid Database 2002-2004., Tasneem Taher Lokhandwala
Do Statins Improve Outcomes In Patients With Asthma On Inhaled Corticosteroid Therapy? A Retrospective Analysis Of The Mississippi Medicaid Database 2002-2004., Tasneem Taher Lokhandwala
Electronic Theses and Dissertations
Animal model studies and clinical trials have looked at the potential benefits of the anti-inflammatory properties of statins in asthma management with contradictory results. Therefore, the objective of this study is to determine if asthma patients on concurrent statin therapy are less likely to have asthma-related hospitalizations and emergency room (ER) visits. We conducted a retrospective cohort study using Medicaid data for 2002–2004. Asthma patients ?18 years old were identified using the ICD9 code 493.xx, from Jul 1, 2002 through Dec 31, 2003. The index date for an exposed subject was any date within the identification period, 180 days prior …
The Relationship Between Psychological Contract Breach, Professional Identity, And Organizational Citizenship Behaviors: An Equity Sensitivity Perspective, Leigh Ann Bynum
Electronic Theses and Dissertations
Objectives: The purpose of this research was twofold. First, it tested the effects of the type of perceived psychological contract breach, equity sensitivity, and identity salience on an important employee outcome, namely organizational citizenship behaviors. Second, the research explored the effects that discipline and pharmacist status have on organizational citizenship behaviors. More precisely, the effect of equity sensitivity on the relationships between identity salience (discipline or school), type of perceived contract breach (administrative or professional) and the performance of organizational citizenship behaviors toward the School of Pharmacy by pharmacy school faculty was examined. Methods: Existing organizational citizenship, identity salience and …