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 20 for “"structure-activity relationship study"”.
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A Structure-Activity Relationship Study of Dihydroajoenes as Anti-Cancer Agents
… known to possess in vitro and in vivo anticancer activity based on the presence of a vinyl disulfide as its pharmacophore. This thesis reports on the synthesis of dihydroajoenes, a novel set of ajoene analogues, containing a saturated double bond, in which the intention was to study the influence …
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Isolation, Synthesis and Structure-Activity Relationship Study of Anticancer and Antimalarial Agents from Natural Products
… fourteen novel compounds with antiproliferative activity against the A2780 human ovarian cancer line. One extract with antimalarial activity was studied, which led to the isolation of two new natural products with antiplasmodial activity against a drug-resistant Dd2 strain of Plasmodium …
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Improving Potency and Oral Bioavailability of Spinster Homolog 2 (Spns2) Inhibitor: A Structure-Activity Relationship Study
In healthy individuals, the autoimmune system is the body's natural defense against foreign materials and organisms. The main tools utilized for this defense mechanism are immune cells. However, in patients suffering from autoimmune diseases, the autoimmune system is overactive resulting in its …
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A Structure-Activity Relationship Study with Isoquinolinone Compounds and Stromal Antigen 2 Mutant Ewing’s Sarcoma Cells and Synthesis of Small Molecules for Anticancer Activity Through TEAD Palmitoylation Inhibition
… The first section will be focused on the structure-activity relationship study with isoquinolinone compounds, and the second on the synthetic approach to small molecules that inhibit the growth of cancer cells through the Hippo signaling pathway. Ewing’s sarcoma is the second most commonly …
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Development of Potent Inhibitors of the Sphingosine-1-Phosphate Transporter Spns2 for the Treatment of Multiple Sclerosis
… potent Spns2 inhibitors are disclosed. These structures spanned several scaffolds and culminated in the discovery of a phenylurea derivative 4.11i. In vitro assessment of 4.11i demonstrated that the compound possessed an IC50 value of 92 nM, making it the most potent inhibitor of Spns2 …
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Synthesis of Sphaeropsidin a Derivatives in a Search for Compounds Active Against Drug-Resistance Cancer
… new chemical agents with promising anticancer activity. One such agent is Sphaeropsidin A (SphA), a fungal metabolite extracted from different sources but mainly from Diplodia cupressi. SphA has shown anticancer activity by overcoming multidrug resistance as well as inducing apoptosis (cell …
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Developing Sphingosine-1-Phosphate (Spns2) Inhibitors for the Treatment of Multiple Sclerosis
Autoimmune diseases are caused when a person's immune system attacks its own healthy cells. In a person with multiple sclerosis, their immune system becomes sensitized to the myelin sheath that covers their neurons in the central nervous system. This results in the degradation of the myelin sheath …
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Chemical Mutagenesis for the Modulation and Study of Protein Function and Dysfunction within Alzheimer’s Disease
… of utilizing chemical mutagenesis to enable a structure-activity relationship study on a single-domain antibody (SdAb) beyond the 20 canonical AAs. The starting SdAb was designed to target the Amyloid-b peptide (Ab) and has a nascent ability to inhibit its aggregation, a key pathological …
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Discriminative stimulus properties of 3-substituent rimonabant analogs
… (e.g., THC) dose-dependently decrease locomotor activity and body temperature and produce antinociception and catalepsy. Drugs that produce this tetrad of effects within a limited dose range are likely to function as CB1 receptor agonists. A structure activity relationship study from our …
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Synthesis and Structure Activity Relationship Studies of a Natural Product-Derived Compound Library
… of finding a new compound with antimicrobial activity.</p> <p>Herein is described a compound library derived from the natural product, nonactin. A preliminary library was previously synthesized by Phillips that yielded two lead compounds that were the starting points for this work. The lead …
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Synthesis and Structure Activity Relationship Studies of a Natural Product-Derived Compound Library
… of finding a new compound with antimicrobial activity.</p> <p>Herein is described a compound library derived from the natural product, nonactin. A preliminary library was previously synthesized by Phillips that yielded two lead compounds that were the starting points for this work. The lead …
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Structure-Activity Relationship Studies of Imidazo[4,5-b]pyrazine Derivatives as Mitochondrial Uncouplers and their Potential in the Treatment of Obesity
… synthesize 1H-imidazo[4,5-b]pyrazines to perform structure-activity relationship studies. Thus, a library of 75 compounds was synthesized and characterized for mitochondrial uncoupling activity. The biological activity of the compounds was demonstrated in oxygen consumption rate assays affording …
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Identification, characterization and bioevaluation of a bioactive peptide from the skin secretion of the Chinese forest frog
… peptides, which is worthy of further study.<br/><br/>In this study, the skin secretions of the Chinese forest frog (Rana chensinensis) were collected in a mitigating stimulation method. Then the natural antimicrobial peptide QUB-1735 was identified by molecular cloning, chromatographic …
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Studies on the Synthesis, Function, and Properties of Troponoids
… elements of the enzyme active site. This study allowed us to refine our inhibitor design; leading to the discovery of a new class of fluorescent small molecule sensors. We also identified crucial deficiencies in our understanding of tropolone structural properties, necessary to the …
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Structure-Activity Relationship Studies of Sphingosine Kinase Inhibitors and Mitochondrial Uncouplers
… which differ with respect to their cellular activity and localization. As the key mediators in the synthesis of S1P, SphKs have attracted attention as viable targets for pharmaceutical inhibition. To validate their potential as therapeutic targets, we aimed to develop potent, selective, and …
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Structure Activity Relationship Studies on Isoform Selective Sphingosine Kinase Inhibitors
… overall compound length. More importantly, this study identified the internal aryl ring of SLR080811 as a key pharmacophore of the scaffold. To further probe the significance of the aromatic region, the phenyl ring was replaced by a 2,6-naphthyl ether skeleton. Investigations into the tail region …
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The Design, Synthesis, and Evaluation of (I) Arylpiperazines and (II) Pyrazolopyrimidinones as potential anti-diabetic agents
… them for their anti-diabetic biological activity. The first family investigated was the arylpiperazine family, which consisted of analogues of the hit compound RTC1. Here, structural variations were performed at five sites on RTC1. The second family explored was the pyrazolopyrimidinone …
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Synthesis of Novel Amino Acids and Peptidomimetics as Tools for Drug Discovery
… tools for drug discovery. The first part of this study focuses on the preparation of modified tyrosine analogues using metal-catalysed coupling reactions and the incorporation of these novel amino acid building blocks into biotin-R8ERY* peptidomimetics using Fmoc SPPS. The second part deals with …
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Developing C–H bond Functionalization, Organocatalytic Hydrophosphination Reactions and Anti-Invasion Agents
… of their distinct chemical properties and reactivity patterns compared to 4d and 5d metals. Several reported monometallic iron imido MLMB species capable of nitrene group transfer do so by accessing high-spin states, although their instability limits their applications. Bimetallic species …
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Design, Synthesis, Biological Evaluation And Molecular Modeling Studies Of Novel Multifunctional Neuroprotective Drugs For The Treatment Of Parkinson's Disease: An Effort Towards The Improvement Of In Vivo Efficacy And Modulation Of Alpha Synuclein Aggregation Property Of The Neuroprotective Parent
… treatment of this disease. Our aim in the first study was to enhance brain penetration of one of our lead molecule D-264. Our current structure activity relationship study is focused on introduction of methoxy and hydroxyl group at various positions on the accessory binding biphenyl ring of this …