Date of Award
8-1-2013
Document Type
Campus Access Thesis
Degree Name
Master of Science (MS)
Department
Chemistry
First Advisor
Béla Török
Second Advisor
Marianna Török
Third Advisor
Jonathan Rochford
Abstract
Several diverse group of molecules were designed and synthesized to test their biological potential as Phospholipase D (PLD) inhibitors and anti-Alzheimer’s disease agents. Phosphatidic acid (PA), known as an important precursor for many essential cellular molecules, is a product of cleavage of glycerophospholipids substrates by PLD enzymes. Overexpression of PLD has been found in several human cancers. PLD inhibitors based on 1,3-disubstituted-4-amino-pyrazolopyrimidine core structure were synthesized and exhibited strong inhibition of the purified PLD enzyme with IC50 values in the nanomolar range. The other target, Alzheimer’s disease is the most prevalent neurodegenerative disorder associated with the loss of cholinergic neurotransmission and the presence of amyloid deposits and neurofibrillary tangles in the brain. Several designed sulfonamide, chalcone and coumarin derivatives showed excellent inhibition of cholinesterases (AChE, BuChE), amyloid beta (Aβ) self-assembly and the disassembled preformed Aβ oligomers and fibrils.
Recommended Citation
Zhou, Weihong, "Design and Synthesis of Bioactive Compounds and their Application in Protein Self-Assembly and Enzyme Inhibition Studies" (2013). Graduate Masters Theses. 197.
https://scholarworks.umb.edu/masters_theses/197
Comments
Free and open access to this Campus Access Thesis is made available to the UMass Boston community by ScholarWorks at UMass Boston. Those not on campus and those without a UMass Boston campus username and password may gain access to this thesis through resources like Proquest Dissertations & Theses Global or through Interlibrary Loan. If you have a UMass Boston campus username and password and would like to download this work from off-campus, click on the "Off-Campus UMass Boston Users" link above.