Publication Date

2016

Document Type

Dissertation/Thesis

First Advisor

Hagen, Timothy J.

Degree Name

Ph.D. (Doctor of Philosophy)

Department

Department of Chemistry and Biochemistry

LCSH

Flavonoids||Urease--Inhibitors||Antimalarials||Aminopeptidases--Inhibitors||Organic chemistry||Biochemistry

Abstract

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).

Comments

Advisors: Timothy J. Hagen.||Committee members: Melvin R. Duvall; James R. Horn; Douglas A. Klumpp; Victor V. Ryzhov.

Extent

389 pages

Language

eng

Publisher

Northern Illinois University

Rights Statement

In Copyright

Rights Statement 2

NIU theses are protected by copyright. They may be viewed from Huskie Commons for any purpose, but reproduction or distribution in any format is prohibited without the written permission of the authors.

Media Type

Text

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