Author/Authors :
Baihua Hu، نويسنده , , James W. Jetter، نويسنده , , Jay E. Wrobel، نويسنده , , Thomas M. Antrilli، نويسنده , , Jean S. Bauer، نويسنده , , Li Di، نويسنده , , Sergiusz Polakowski، نويسنده , , Uday Jain، نويسنده , , David L. Crandall، نويسنده ,
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.
