Hagen, Timothy J.
Ph.D. (Doctor of Philosophy)
Department of Chemistry and Biochemistry
Flavonoids; Urease--Inhibitors; Antimalarials; Aminopeptidases--Inhibitors; Organic chemistry; Biochemistry
This dissertation explores the inhibition of prominent enzymatic pathways important for both medicinal and agricultural applications. The research involved three distinct projects: First, an enzymatic urease inhibitory assay was optimized for plate-based screening of tree bark extracts to compare with ex vivo results from simulated-barn floor manure slurry assays performed by Dr. Wayne Zeller (USDA, Madison, WI). It wafs discovered that the measured ammonia abatement activities of each extract exhibited a correlation in both the enzymatic and ex vivo assays. Second, aminoalkylated quercetin analogs were synthesized and screened for antimalarial activity. The most potent species were found to exhibit sub-micromolar inhibitory values against multidrug-resistant strains of Plasmodium falciparum, the malarial parasite. Finally, a library of potential inhibitors of methionine aminopeptidase, an enzyme necessary for bacterial proliferation, were synthesized or purchased and screened for enzymatic inhibitory activity. A number of sub-micromolar inhibitors were discovered, and the most potent compounds were screened in a host-cell viability assay by Dr. Jonathon Audia (USA, Mobile, AL).
Helgren, Travis Robert, "The utilization of flavonoids as inhibitors of urease and as antimalarial agents and the discovery of bacterial methionine aminopeptidase inhibitors" (2016). Graduate Research Theses & Dissertations. 6388.
Northern Illinois University
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