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Dissertation/Thesis Abstract

Organophosphate Triester Inhibitors of Butyrylcholinesterase: Part I: Effect of Cholinyl Substituent. Part II: Effects of the Substitution of Oxygen by Sulfur Atoms
by Ly, Phillippe K., M.S., California State University, Long Beach, 2020, 131; 27742418
Abstract (Summary)

Butyrylcholinesterase (BuChE) is known to show increased activity in patients with Alzheimer’s Disease and likely contributes to the symptomatic decline in cognition. Therefore, it is an attractive goal to develop a synthetic drug that is highly specific for inhibiting BuChE. Herein, we build upon previous organophosphorus inhibitor designs by changing substituents on the phosphorus center in two ways: 1) the addition of substrate features to mimic the cationic-pi interaction, and 2) the substitution of oxygen for sulfur atoms to incorporate a better leaving group. However, for the former, stereochemistry on the phosphorus center was also evaluated for using enantiomerically enriched mixtures. Herein, the synthesis, purification, and biological characterization of a library of inhibitors are detailed. The results of these experiments increase our understanding of the molecular interactions between the potential drug candidate and its target and inform us on how to design more potent, target-specific drugs.

Indexing (document details)
Advisor: Nakayama, Kensaku
Commitee: Schwans, Jason, McAbee, Douglas
School: California State University, Long Beach
Department: Chemistry and Biochemistry
School Location: United States -- California
Source: MAI 81/12(E), Masters Abstracts International
Subjects: Biochemistry, Organic chemistry
Keywords: Butyrylcholinesterase, Organophosphate, Sulfur substitution
Publication Number: 27742418
ISBN: 9798661681379
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