Design, synthesis, and biological evaluation of non-symmetric smal

<p>Plasminogen activator inhibitor-1 (PAI-1) is a member of the serpin family of proteins, a primary inhibitor of both tissue-type and urokinase-type plasminogen activators in plasma, and is a well-established risk factor in various disease conditions. Increased levels of active PAI-1 in plasma are correlated with the development of atherosclerosis, diabetes, stroke, and other maladies. In the present study, we describe the synthesis of two new series of compounds that aim to reduce physiologically active PAI-1 levels. These molecules are related to a series of bis-arylsulfonimides and arylsulfonamides connected by short linking diamines, and to a series of hydrazine-based analogues. These studies resulted in the identification of small molecule inhibitors of PAI-1 that displayed <em>in vitro</em> IC₅₀ values in the low micromolar range.</p>

Name thesis:degree_name

Master of Science (MS)

Level thesis:degree_level

Open Access Thesis

Discipline thesis:degree_discipline

Chemistry

Year dc:date.available

2014

Author dc:creator

• Anumala, Himabindu

Contributors dc:contributor

• Cory Emal, PhD, Chair
• Gregg Wilmes, PhD
• Steven Pernecky, PhD

• Chemistry

Repository record dc:identifier

https://commons.emich.edu/theses/701

OAI identifier oai:identifier

oai:commons.emich.edu:theses-2080