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 “"chemotype"”.
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Hemiaminals : a new chemotype for organocatalysis
Jorgensen and List introduced enantioselective α-amination of an aldehyde with an azodicarboxylate as the electrophile using L -proline enamine catalysis in 2002. Following borohydride reduction, the α-hydrazino alcohol was obtained in high yield (93-99%) and enantioselectivity (86-97%). …
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Synthesis of 1,4 Dihydropyridines as potential antimalarial chemotype
The blood stage of the malarial parasite life-cycle is a vital stage that is believed to be a target for most antimalarial drugs. It is in this stage that host haemoglobin is degraded to provide nutrients for the survival of the parasite. However, a pathway (known as the haem detoxification …
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Investigation of Dual Stage Acridones as a Potent Malaria Treatment
… is urgent. Discovery of novel acridone chemotypes have shown promise for a new antimalarial drug treatment. Presently, two acridone chemotypes have intrinsic antimalarial potency against chloroquine sensitive and multidrug resistant parasites. Acridones lacking an N10 side chain are …
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Thymus pulegioides chemotipai Lietuvoje: paplitimas, edafinių ir klimatinių salygų įtaka, alelopatinės savybės /
The regularities of the distribution of different chemotypes of large thyme (Thymus pulegioides) in Lithuania, influence of edaphic and climatic factors on quantitative and qualitative composition of essential oils, as well as allelopathic and autoallelopathic effect of different chemotypes were …
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On Two Problems in Comparative Genomics of Eukaryotes
… strains comprise two mutually-exclusive toxin chemotypes, one producing satratoxins (a subclass of trichothecenes) and the other producing the less-toxic atranones. To determine the genetic bases for chemotype-specific differences in toxin production, I sequenced and assembled de novo four …
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The development of small molecule inhibitors for fibrosis drug discovery
… inhibitors for ATX have resembled the lipid chemotype of the native ligand; however, a small number of inhibitors have been described that deviate from this common scaffold. Herein, Chapter 1 details the structure-activity relationship (SAR) exploration of a previously reported small molecule …
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Approaches to lead generation for idiopathic pulmonary fibrosis targets
… a scaffold hopping approach, a more minimalistic chemotype was identified with improved physicochemical properties. In the PF-8380 derived series, a structure-based drug design approach was undertaken to fully understand binding interactions involved in ATX inhibition. Using biostructural and …
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The Design and Synthesis of β-Keto Vinyl Sultams and Macrocyclic β-Keto Vinyl Sultams: Novel Analogs of Tetramic Acids
… core structural motif have emerged as a rich chemotype due to their potent and broad biological activities. Several bioactive tetramic acid-containing compounds have been reported with a variety of activities, including antibacterial, anticancer and anti-inflammatory activities, as well as …
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The interaction of antimicrobial peptides with lipopolysaccharide aggregates and model membranes.
… LPS monomers. The intact LPS molecule (smooth chemotype) forms elongated micelles in solution whereas truncated LPS molecules (rough chemotypes) form lamellar aggregates. Biological toxicity tests revealed that the dierent chemotypes have dierent toxic activities on cultured macrophage cells. …
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Medicinal Chemistry of Cannabis and Cannabinoids
… effects on receptors vary significantly with chemotype and in turn reflects their chemical compositions. Several first-in-kind studies detailed in this thesis pave the way for further investigations of cannabinoids into their chemical structures, mechanism(s) of receptor binding, as well as …
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Optimization of N-(1-Adamantyl)-3-Aryl Acetamides as Novel Antimycobacterial Agents
… data support further optimization of this novel chemotype for the treatment of Mtb infections.
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Structure guided discovery of inhibitors of indoleamine 2,3-dioxygenase (IDO1)
… compounds as a novel IDO1 inhibitory chemotype that may be a useful scaffold for the further lead development.
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Synthesis and profiling of antimalarial side-chain modified pyrido[1,2-a]benzimidazoles
… studies were carried out on a novel antimalarial chemotype, namely the pyrido[1,2-a]benzimidazoles (PBI) class of compounds. A frontrunner compound based on the PBI scaffold was previously found to possess potent antiplasmodial activity in vitro [IC₅₀(Pf NF54) = 0.11 μM; IC₅₀(Pf K1) = 0.12 μM] and …
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Analyzing Resistance to Design Chemical Inhibitors of AAA Proteins
<p>Chemotype-specific resistance is a major factor limiting the efficacy of molecularly targeted therapeutics. Analyses of resistance mechanisms to drugs reveal that mutations conferring resistance often arise in the drug's binding sites. As selective binding of inhibitors to their protein targets …
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Design of Selective Plasmodium falciparum Kinase Inhibitors using Computer-Aided Drug Discovery
… PfPKG inhibition by compounds belong to this chemotype. Using chemoinformatic approaches, compounds from an in-house imidazopyridazine library were prioritised for PfPKG inhibition assays to validate molecular docking findings and understand protein-inhibitor interactions important for PfPKG …
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Rational Development of New Inhibitors of Lipoteichoic Acid Synthase
… simulations, I have discovered a new inhibitor chemotype that seems to exhibit a different mode of action against eLtaS. Taken together, my work presents a computational platform for future drug design against eLtaS and reinforces the notion that targeting eLtaS is a viable strategy to combat …
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Ecological Perspectives on Cannabis sativa Phytochemistry: Biotic Interactions and Abiotic Stress in Managed and Natural Systems
… the most consistent insect associates across chemotypes and regions. Cultivated hemp supported the highest morphospecies richness, followed by cultivated marijuana and feral hemp. Most morphospecies occurred in only one location or chemotype-region combination, indicating high spatial turnover …
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Physicochemical, biological and β-haematin inhibiting activity of pyrido-dibemequines, pyrido[1,2-α]benzimidazoles and their derivatives
… broad antimicrobial potency of this chemotype.
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Design, synthesis, and structure-activity relationship studies of dual Plasmodium falciparum phosphatidylinositol 4-kinase and cGMP-dependent protein kinase inhibitors
… kinase (PKG) inhibitors, based on two distinct chemotypes. Plasmodium PI4K and PKG are validated targets, each with the potential to deliver pan-stage active compounds with potentially moderate to low risk of resistance. Part 1 of this study focused on the repositioning of the oncological …
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Distribution of chemistry and sexual fecundity in the lichenized-fungi, Xanthoparmelia cumberlandia and Xanthoparmelia coloradoensis on Boulder Mountain, Aquarius Plateau, UT
… are supported by distinct differences in their chemotypes (combinations of secondary chemicals). Norstictic acid, which the literature also associates with <em>X. cumberlandia</em>, is found frequently in both<em> X. cumberlandia</em> and <em>X. coloradoënsis</em>, and is not a good …