Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1367953 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
We synthesized and evaluated a novel series of 2-carboxylic acid indole-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). Systematic modification of the N-1 position and the 5-position of the indole scaffold resulted in the identification of several compounds that showed good potency against PAI-1 in the spectrophotometric assay. This potency did not always translate to the antibody assay. Solubility and serum protein binding studies on selected analogs revealed that protein binding might be a factor in the poor correlation between the two assays.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Baihua Hu, James W. Jetter, Jay E. Wrobel, Thomas M. Antrilli, Jean S. Bauer, Li Di, Sergiusz Polakowski, Uday Jain, David L. Crandall,