Plasminogen activator inhibitor-1 (PAI-1) is a mammalian serine protease inhibitor and a key regulator of fibrinolysis. Individuals in certain disease states experience higher levels of active PAI-1, resulting in an increased risk of thrombosis and embolism. Reduction of circulating active PAI-1 levels by use of an appropriate PAI-1 inhibitor may therefore decrease this risk. The focus of this research is to explore a novel class of PAI-1 inhibitors identified from a dual-reporter high-throughput screen. Here we present initial data related to the structure-activity relationships of these hydrazide-containing inhibitors in a plasma-based assay system.

Design, synthesis, and evaluation of novel hydrazide-based small-molecule inhibitors of plasminogen activator inhibitor-1

248th National Meeting (2014)

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