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Articles 1 - 7 of 7
Full-Text Articles in Medicine and Health Sciences
Structure-Activity Relationship And Mechanistic Studies On The Chemopreventive Activity Of Dipyridamole And Its Analogues, Ja’Wanda Shavon Grant
Structure-Activity Relationship And Mechanistic Studies On The Chemopreventive Activity Of Dipyridamole And Its Analogues, Ja’Wanda Shavon Grant
Theses and Dissertations (ETD)
There is an escalating demand in the area of cancer prevention and control for the development of novel agents and molecular targets that have potential to reduce the incidence of cancer. In this study, the JB6 mouse epidermal cell-culture based transformation model was used in efforts to identify novel chemopreventive agents and targets. The nucleoside transport inhibitor dipyridamole (DPM) showed potent chemopreventive activity against JB6 P+cells (tumor promotion sensitive). To probe the effects of DPM structural features on its antitumor promotion activity, the soft-agar colony forming efficiency assay was used to screen an in-house library of …
Structure- And Ligand-Based Design Of Novel Antimicrobial Agents, Kirk Edward Hevener
Structure- And Ligand-Based Design Of Novel Antimicrobial Agents, Kirk Edward Hevener
Theses and Dissertations (ETD)
The use of computer based techniques in the design of novel therapeutic agents is a rapidly emerging field. Although the drug-design techniques utilized by Computational Medicinal Chemists vary greatly, they can roughly be classified into structure-based and ligand-based approaches. Structure-based methods utilize a solved structure of the design target, protein or DNA, usually obtained by X-ray or NMR methods to design or improve compounds with activity against the target. Ligand-based methods use active compounds with known affinity for a target that may yet be unresolved. These methods include Pharmacophore-based searching for novel active compounds or Quantitative Structure-Activity Relationship (QSAR) studies. …
Synthesis And Evaluation Of Tetramic Acids As Antimicrobial Agents, Jason B. Wilson
Synthesis And Evaluation Of Tetramic Acids As Antimicrobial Agents, Jason B. Wilson
Theses and Dissertations (ETD)
As bacterial infectious diseases are a major cause of morbity and mortality throughout the world, and many causative organisms are resistant to currently available antibiotics, the motivation for the development of new drugs is readily apparent. A number of natural products exhibiting antimicrobial activity possess a tetramic acid (2,4-pyrrolidinedione) functional group. As their antibacterial mechanism of action is different from that of many of the currently available antibiotics, these compounds have potential to serve as a basis for a pharmacophore in synthetic compounds. However, toxicity to eukaryotic cells is frequently a problem with currently known tetramic acids. The purpose of …
Controlled Release Of Insulin And Modified Insulin From A Novel Injectable Biodegradable Gel, Om Anand
Controlled Release Of Insulin And Modified Insulin From A Novel Injectable Biodegradable Gel, Om Anand
Theses and Dissertations (ETD)
The objective of the study was to develop a controlled release dosage form of
insulin, which can provide basal concentrations of insulin in diabetic rats for 1 to 2 weeks after a single subcutaneous injection.
A biodegradable injectable drug delivery gel was prepared by dissolving a
biodegradable polymer, polylactic-co-glycolic acid (PLGA), in biocompatible
plasticizer(s), triethyl citrate (TEC) and/or acetyl triethyl citrate (ATEC). Insulin was
then loaded into the blank gel to form an insulin suspension in the polymer solution.
After the insulin-loaded gel was injected subcutaneously, the plasticizer(s) dissolved in the aqueous media and were gradually taken away from the …
Design, Synthesis, And Evaluation Of Small Molecules In The Discovery Of Novel Antimicrobial Agents, Kimberly D. Grimes
Design, Synthesis, And Evaluation Of Small Molecules In The Discovery Of Novel Antimicrobial Agents, Kimberly D. Grimes
Theses and Dissertations (ETD)
The increasing prevalence of antibiotic-resistant bacteria, including Mycobacterium tuberculosis, Streptococcus pneumoniae, Staphylococcus aureus, and Enterococcus faecalis, pushes us to discover new antibacterial agents to maintain adequate patient coverage. This body of work highlights the use of medicinal chemistry methodologies that encompass cross-disciplinary fields of study. Chapter 1 gives an introduction to the antibacterial drug targets, resistance, and how scientists are working to overcome obstacles encountered with drug-resistant bacteria. It also details modern medicinal chemistry applications in antimicrobial drug discovery. Chapter 2 details the use of a structure-guided library approach to drug design, in which large virtual libraries against the target …
Why Pharmacists Choose To Seek Or Not Seek Board Certification In Pharmacy Practice: A Comparison Of Motivation And Motivating Factors, Mark Tankersley
Why Pharmacists Choose To Seek Or Not Seek Board Certification In Pharmacy Practice: A Comparison Of Motivation And Motivating Factors, Mark Tankersley
Theses and Dissertations (ETD)
The stated mission of the Board of Pharmaceutical Specialties (BPS) with regard to specialization is, via board certification, to recognize specialty areas, define skill standards for those specialty areas, and evaluate the knowledge and skills of individual Pharmacy specialists. The perceived or real benefits to the pharmacist of pursuing board certification are unknown. These benefits can be evaluated by separating into values (valences) and instrumentalities, the latter of which is the perceived or known probability that a performance will lead to an outcome. The primary purpose of this study was to determine the differences in values and instrumentalities perceived by …
Flavonoids And Related Compounds As Nucleoside Transporter Inhibitors, Surekha Ravaji Pimple
Flavonoids And Related Compounds As Nucleoside Transporter Inhibitors, Surekha Ravaji Pimple
Theses and Dissertations (ETD)
Mammalian nucleoside transporters can be classified into two main categories, namely, equilibrative nucleoside transporters (ENTs) and concentrative nucleoside transporters (CNTs). ENTs are ubiquitous, and mediate sodium-independent bi-directional facilitated diffusion nucleoside transport processes. CNTs on the other hand, are secondary active unidirectional transporters that are sodium-dependent. Both the equilibrative and the concentrative nucleoside transporters have several family members which are ENT1 to ENT4 and CNT1 to CNT6. Over the past two decades, important advances in the understanding of nucleoside transporter functions have been made. Identification and molecular cloning of the ENT and CNT families from mammals and protozoan parasites have provided …