Date Approved
2008
Degree Type
Open Access Thesis
Degree Name
Master of Science (MS)
Department or School
Chemistry
Committee Member
Cory Emal, PhD, Chair
Committee Member
Harriet Lindsay, PhD
Committee Member
Gregg Wilmes, PhD
Abstract
This work describe the design, synthesis and evaluation of small-molecule inhibitors of two different biological targets: Plasmodium falciparium, the most virulent malarial parasite in humans, and plasminogen activator inhibitor-1 (PAI-1), an endogenous serine proteases inhibitor implicated in a wide range of biological processes. Malaria is one of the top global health threats, and there is a great need for developing effective new chemotherapies. PAI-1 is a major component in the regulation of the plasminogen activation system, and the overexpression of this protein has been implicated in a number of conditions, such as thrombosis, atherosclerosis, and myocardial infarction. The research discussed concerns the design and synthesis of enantiomerically pure anti-malarial compounds containing chiral 1,2-aminoalcohol moiety. In addition, the synthesis and biological evaluation of several highly potent, novel, polygalloyl PAI-1 inhibitors based on common carbohydrates and tethers of various lengths is also presented.
Recommended Citation
Puscau, Maria Mirela, "Design and synthesis of small-molecule inhibitors as anti-malarial and anti-serpin agents" (2008). Master's Theses and Doctoral Dissertations. 156.
https://commons.emich.edu/theses/156