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.
","abstract_html":"<p>This work describe the design, synthesis and evaluation of small-molecule inhibitors of two different biological targets: <em>Plasmodium falciparium</em>, 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.</p>","abstract_has_math":false,"creators":["Puscau, Maria Mirela"],"institution":null,"degree_name":"Master of Science (MS)","degree_level":"Open Access Thesis","degree_discipline":"Chemistry","degree_department":null,"school":null,"contributors":["Cory Emal, PhD, Chair","Harriet Lindsay, PhD","Gregg Wilmes, PhD"],"advisors":[],"committee_chairs":[],"committee_members":[],"year":2008,"date_issued":"2008-01-01T08:00:00Z","date_published":"2008-01-01T08:00:00Z","updated_at":"2026-07-24T02:16:30Z","subjects":["Antimalarials Research","Antiparasitic agents","Malaria Treatment","Chemistry"],"languages":[],"rights":[],"rights_urls":[],"identifier_entries":[]},"links":{"outbound_url":"https://commons.emich.edu/theses/156","outbound_label":"Repository record","outbound_source":"dc:identifier"},"metadata_groups":[{"id":"people","label":"People","entries":[{"key":"dc:contributor","label":"Contributor","values":["Cory Emal, PhD, Chair","Harriet Lindsay, PhD","Gregg Wilmes, PhD"]},{"key":"dc:creator","label":"Author","values":["Puscau, Maria Mirela"]}]},{"id":"academic_context","label":"Academic Context","entries":[{"key":"thesis:degree_discipline","label":"Discipline","values":["Chemistry"]},{"key":"thesis:degree_level","label":"Degree Level","values":["Open Access Thesis"]},{"key":"thesis:degree_name","label":"Degree Name","values":["Master of Science (MS)"]}]},{"id":"subjects_keywords","label":"Subjects and Keywords","entries":[{"key":"dc:subject","label":"Dc Subject","values":["Antimalarials Research","Antiparasitic agents","Malaria Treatment","Chemistry"]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier","label":"Identifier","values":["https://commons.emich.edu/theses/156"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description.abstract","label":"Abstract","values":["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.
"]},{"key":"dc:title","label":"Title","values":["Design and synthesis of small-molecule inhibitors as anti-malarial and anti-serpin agents"]}]}],"canonical_facts":{"dc:contributor":["Cory Emal, PhD, Chair","Harriet Lindsay, PhD","Gregg Wilmes, PhD"],"dc:creator":["Puscau, Maria Mirela"],"dc:description.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.
"],"dc:identifier":["https://commons.emich.edu/theses/156"],"dc:subject":["Antimalarials Research","Antiparasitic agents","Malaria Treatment","Chemistry"],"dc:title":["Design and synthesis of small-molecule inhibitors as anti-malarial and anti-serpin agents"],"thesis:degree_discipline":["Chemistry"],"thesis:degree_level":["Open Access Thesis"],"thesis:degree_name":["Master of Science (MS)"]},"updated_at":"2026-07-24T02:16:30Z"}