Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 195 for “"medicinal chemistry"”.
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Medicinal Chemistry of Cannabis and Cannabinoids
… pre-clinical level, drawing on core aspects of medicinal chemistry and applying developed techniques under large study settings. Through pilot experiments, extraction protocols for the optimal recovery of cannabinoids from different types of cannabis plant material were investigated and the …
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Chiral alkaloid derivatives: Synthesis and medicinal chemistry applications
The preparation of a selection of novel opioid alkaloids based on alteration at the 1, 3 and 6 positions of codeine and morphine has been achieved. Herein we present the synthetic methodology, structural characterisation and biological evaluation of these novel opioid species. A range of opioid …
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Biosynthesis and medicinal chemistry of therapeutically promising plant natural products
… that possess pharmacological activity from medicinal plants. While approximately 50% of all new FDA-approved small molecule therapeutics in the past 40 years were natural products or natural product analogs, challenges including limited natural resources and the difficulty of solving the …
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Development of computational tools to model molecular interactions for medicinal chemistry
Medicinal chemistry has evolved over the past 40 years to rely heavily on the computationally aided design of new drugs. The work in this dissertation focuses on developing computational tools for the application of medicinal chemistry. For computational techniques to be dependable, important …
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Enzymology And Medicinal Chemistry Of N5-Carboxyaminoimidazole Ribonucleotide Synthetase : A Novel Antibacterial Target
<p>N5-Carboxyaminoimidazole ribonucleotide synthetase (N5-CAIR synthetase), a key enzyme in microbial de novo purine biosynthesis, catalyzes the conversion of aminoimidazole ribonucleotide (AIR) to N5-CAIR. To date, this enzyme has been observed only in microorganisms, and thus, it represents an …
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A medicinal chemistry approach to drug repositioning in the treatment of tuberculosis and malaria
… agent metergoline, in TB and/or malaria via medicinal chemistry approaches. New semisynthetic derivatives of fusidic acid and metergoline were synthesized and evaluated for antimycobacterial activity against the H37Rv strain of Mtb and antiplasmodial activity against the NF54 strain of P. …
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Antimalarial benzimidazoles and related structures incorporating an intramolecular hydrogen bonding motif: medicinal chemistry and mechanistic studies
Malaria, an infectious disease caused by Plasmodium parasites, continues to take an enormous toll on human health, particularly in tropical regions. According to the World Health Organization (WHO), progress against malaria eradication has stalled, specifically in the African region. Global efforts …
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Platinum group metal coordination complexes of ferrocenyl N-donor ligands and their potential application in catalysis and medicinal chemistry
In this project a series of multinuclear complexes were successfully prepared and characterised using an array of analytical techniques. The use of nitrogen-donor ligands, in particular pyridine and ferrocenyl derivatives thereof was examined. Two main approaches were taken in the preparation of …
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Structure-Based Drug Design in Medicinal Chemistry I. Development of Translesion Synthesis Inhibitors II. Synthesis and Biological Evaluation of Sulfonyl Piperazine Derivatives for LpxH Inhibition
<p>The identification of a promising lead compound is a crucial step for the drug development. Despite of a number of approaches, the optimization of promising hit compounds is still challenging. Structure-based drug design approach is a well established and widely used strategy based on the 3D …
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Design, Synthesis, and Evaluation of Small Molecules in the Discovery of Novel Antimicrobial Agents
… 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 …
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Memory of Chirality in 1,4-Benzodiazepin-2-ones
… synthesis. It has been applied to enolate chemistry, reactions involving carbocation intermediates, and to radical systems. In this strategy the chirality of an enantiopure reactant is transferred to the dynamic chirality of a reactive intermediate to produce stereospecific product. …
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The Development of Assays for Detecting Proximal Phosphorylation and Covalent Modification of Proteins
… research for several disciplines including medicinal chemistry, molecular recognition and chemical biology. Achieving success in bioassays represents important milestones in many pharmaceutical pipelines and disease diagnostics, and as such, must be designed and fine-tuned to produce …
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Synthesis and Molecular Modeling Studies of Bicyclic Inhibitors of Dihydrofolate Reductase, Receptor Tyrosine Kinases and Tubulin
… studies support structure-based and ligand-based medicinal chemistry efforts in order to improve potency and/or selectivity of analogs of the docked compounds against these targets.</p><p> Novel topomer CoMFA models were developed for tgTS and hTS using a set of 85 bicyclic inhibitors and for RTKs …
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Synthesis and evaluation of β-fluoro-γ-aminobutyric acid enantiomers
The impact of fluorine in medicinal chemistry is reviewed in the first chapter of this work and the fluorine gauche effect, which has not been fully exploited in medicinal chemistry, is also discussed. GABAA and GABAB receptors are then presented and the synthesis of neurosteroid antagonists acting …
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Solution equilibria of the methyldopacopper (II) system and the crystal and molecular structures of selected compounds
… system and its relevance to medicinal chemistry, a full abstract of which is given on page 1 of the main text. The second part describes five single crystal x-ray investigations into some interesting compounds isolated at this university. The abstracts to these topics may be …
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The Design and Synthesis of Novel Antimicrobial Agents for Use in the Battle Against Bacterial Resistance
… of work brings to light the many ways in which medicinal chemistry plays a vital role in the discovery of novel antimicrobial agents. Chapter 1 is an introduction into antimicrobial agents. It provides a brief history of the discovery of antimicrobial agents, and delves into reasons why new …
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Synthesis of a Water Soluble Resveratrol Derivative as a Potential Anti-Cancer Drug.
… drugs is one of the great challenges of modern medicinal chemistry. Resveratrol (Res) is one of the many phytoalexins producing stilbenoids present in several medicinal plants, grape skin, peanuts, and red wine. It has been found to exhibit anti-cancer, anti-inflammatory, and anti-oxidant …
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HIV-1 protease as a target for antiretroviral therapy
… of molecular biology, biotechnology, and medicinal chemistry, highlighting the importance revisiting old questions with new approaches. The goal of this thesis is to advance our biochemical knowledge of HIV-I protease and develop novel therapeutics targeting this key viral enzyme. In …
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Probing the mechanisms of action and resistance of mixed-ligand platinum(II) complexes with dual-stage antiplasmodium activity
… This has left the field of inorganic medicinal chemistry and transition metal-based chemotherapeutics underexplored and underrepresented.
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