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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 48 for “"Structure Activity Relationship Studies"”.
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Structure-Activity Relationship Studies of Mitochondrial Uncouplers and PilB Inhibitors
… high uncoupling nature of these compounds. Our structure-activity relationship (SAR) studies demonstrated that the hydroxylamine BAM15 analogs are more potent than hydrazine ones, with particular note of hydroxylamine ester derivatives being the most efficacious of all structures assayed. For …
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Structure Activity Relationship Studies on Isoform Selective Sphingosine Kinase Inhibitors
… described in detail. Key discoveries from this structure-activity relationship study include SLC5111312 (hSphK2 Ki = 0.90 μM, dual hSphK inhibitor), SLC5091592 (hSphK2 Ki = 1.02 μM, > 20-fold hSphK2 selective) and SLC5121591 (hSphK2 Ki = 0.61 μM, >16-fold hSphK2 selective). Molecular modeling …
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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 and biological evaluation of selective sphingosine kinase inhibitors
… become a prevalent drug discovery target due to studies implicating it to several disease pathologies such as fibrosis, sickle cell disease, inflammation, diabetes, and cancer. S1P functions to induce cell proliferation and migration. S1P signaling occurs through intracellular targets or …
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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 2-phenylbenzimidazoles and related organometallic complexes as antiplasmodial agents
… candidates, displaying potent antiplasmodial activity. Furthermore, benzimidazoles can be chemically transformed into metal-containing organometallic complexes that elevate generally flat benzimidazoles to the third dimension. To date, examples of metal-containing benzimidazoles are extremely …
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Submonomer Synthesis and Structure-activity Relationship Studies of Azapeptide Inhibitors of the Insulin Receptor Tyrosine Kinase
… which translates into bio-active secondary structures that improves the pharmacological properties of the native peptide sequence. More specifically, azapeptides contain a semicarbazide within the peptide backbone which restricts the peptide bond torsion angles (<em>φ, ψ</em>) into …
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STRUCTURE–ACTIVITY RELATIONSHIP STUDIES OF HYBRID ANTITUMOR AGENTS FOR THE TREATMENT OF NON-SMALL CELL LUNG CANCER
… dissertation was concerned with establishing structure–activity relationships (SAR) in this novel class of DNA-targeted antitumor agents with the ultimate goal of improving the biological activity of the prototypical agent, PT-ACRAMTU. Two ways were explored of tuning the reactivity and target …
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Branched Peptides Targeting HIV-1 RRE RNA and Structure-Activity Relationship Studies of Spinster Homolog 2 Inhibitors
… stability, potency, selectivity, and in vivo activity for RRE RNA. An unnatural amino acid branched peptide library (46,656 sequences) was synthesized and screened against RRE IIB and several hits in the sub-micromolar regime were found. A number of hits demonstrated selectivity in the …
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Synthesis and structure-activity relationship studies of novel anti-infectives for cross screening in tuberculosis and malaria disease models
… compounds. Of these, 5 showed inhibitory activity in vitro against the parasite at a concentration of 10 μM. Analysis of the data on all the 165 compounds revealed some preliminary structure-activity relationships. Based on this preliminary structure-activity relationship data, compounds …
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Design, synthesis, and structure-activity relationship studies of dual Plasmodium falciparum phosphatidylinositol 4-kinase and cGMP-dependent protein kinase inhibitors
… inhibitor with potent PI4K and PKG inhibitory activity. In this study, an in silico-guided structural modification strategy was undertaken towards optimizing dual Plasmodium kinase inhibition and anti-plasmodium activity while also mitigating potency against its oncological human target, mTOR …
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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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Synthesis and Structure-Activity Relationship Studies of 3-(N-Butylethanimidoyl)-4-hydroxy-2H-chromen-2-one (BHC) Analogues for Myosin II Inhibition
… (BHC), was found to inhibit myosin II. The structure-activity relationship (SAR) study of BHC analogues are performed in this study. To implement the SAR studies of BHC analogues, the synthetic route to complete the Schiff base was developed. The synthesis of 3-acetyl-4-hydroxycoumarin …
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Toward the Synthesis of CAY-1, an Antifungal Steroidal Saponin
… the cayenne pepper plant in 0.1% yield. In Vitro studies of CAY-1 have shown it to be an effective antifungal agent against sixteen pathogenic fungal strains and it showed no cytotoxicity toward mammalian cells up to 100 ìg/mL. The development of a practical synthesis of CAY-1 will potentially …
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Optimization of Receptor-Interacting Protein Kinase 2 (RIPK2) Inhibitors and Development of Mixed Lineage Kinase Domain-Like (MLKL) Activators
… regulatory pathways. Protein kinases’ catalytic activity is critical for controlling a myriad of cellular events and functions. Despite a lack of catalytic activity, pseudokinases have merged as nuanced modulators, scaffolds, and molecular switches in diverse signaling pathways. Chapter one …
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Pleuromutilin and its Application Towards Bidentate Antibiotics: Triazoles, Linker Chemistry, and Serendipitous Discoveries
… which now serve as lead compounds for future structure activity relationship studies and development. Additionally, unexpected activity against P. falciparum has resulted in a new project pursuing pleuromutilin antimalarials.
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New aminoquinoline antimalarial cysteine protease inhibitors based on the isatin natural product scaffold
… Plasmodium Jalciparum (P.f. W2). The results of structure activity relationship studies demonstrate the influence of substituents at position 5 of the isatin scaffold. With respect to the chain length, a two carbon methylene spacer between the aminoquinoline and isatin moieties, was found …
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Bromotyrosine-derived natural products: synthetic and biological studies
… they exhibit a rich variety of chemical structures and display a diverse range of bioactivities which makes them of great interest to both the chemical and biological research communities. This thesis is divided into four Chapters and describes the total syntheses of five …
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