Dissertation/Thesis Abstract

Novel bivalent organophosphates as inhibitors of butyrylcholinesterase — Compounds with potential for treatment of Alzheimer's disease and studies in the development of asymmetric catalytic Kabachnik-Fields reaction
by Tu, Kim Ngan, M.S., California State University, Long Beach, 2013, 98; 1527349
Abstract (Summary)

Part A: Butyrylcholinesterase (BChE) is a nonspecific cholinesterase found in blood plasma with unknown physiological function. BChE, like acetylcholinesterase (AChE), can hydrolyze acetylcholine. Since BChE activity in the brain of Alzheimer's patients is elevated 40-90% above normal, BChE inhibitors can increase acetylcholine concentration in the brain and hold promise in the treatment of Alzheimer's disease. Different structural variations of the bisphosphates were prepared and evaluated in vitro for their inhibitory activity against BChE to determine the optimal linker chain length and the alkyl side chain groups in order to maximize inhibition.

Part B: Different achiral Lewis acid catalysts were screened for the KabachnikFields reaction of aliphatic aldehydes. Phenylboronic acid exhibited good catalytic activity toward the reaction. A chiral boron based catalyst was synthesized and exhibited excellent catalytic activity for Kabachnik-Fields reaction of aliphatic aldehyde. We were also interested in investigating the stereoselectivity of the Kabachnik-Fields reaction using chiral aldehyde.

Indexing (document details)
Advisor: Nakayama, Kensaku
School: California State University, Long Beach
School Location: United States -- California
Source: MAI 52/05M(E), Masters Abstracts International
Subjects: Molecular chemistry
Keywords: Alzheimer's disease, Asymmetric synthesis, Butyrylcholinesterase inhibitor, Dual-site inhibition, Kabachnik-fields reactions, Organophosphates
Publication Number: 1527349
ISBN: 978-1-303-76624-4
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