Date Approved

2008

Degree Type

Open Access Thesis

Degree Name

Master of Science (MS)

Department

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.

Included in

Chemistry Commons

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