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ID: ALA1140369
Journal: Bioorg Med Chem Lett
Title: Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1.
Authors: Hu B, Jetter JW, Wrobel JE, Antrilli TM, Bauer JS, Di L, Polakowski S, Jain U, Crandall DL.
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.
CiteXplore: 15982877