title: Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1.
abstract: A novel series of PAI-1 inhibitors containing an oxadiazolidinedione moiety were identified by high through-put screening. Optimization of substituents by parallel synthesis and the iterative design toward understanding structure-activity relationship to improve potency are described.
authors.affiliation: Chemical and Screening Sciences, Wyeth Research, 401 N Middletown Road, Pearl River, NY 10965, USA. gopalsa@wyeth.com
authors.forename: Ariamala
authors.initials: A
authors.lastname: Gopalsamy
authors.forename: Scott L
authors.initials: SL
authors.lastname: Kincaid
authors.forename: John W
authors.initials: JW
authors.lastname: Ellingboe
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Groeling
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Antrilli
authors.forename: Girija
authors.initials: G
authors.lastname: Krishnamurthy
authors.forename: Ann
authors.initials: A
authors.lastname: Aulabaugh
authors.forename: Gregory S
authors.initials: GS
authors.lastname: Friedrichs
authors.forename: David L
authors.initials: DL
authors.lastname: Crandall
mesh_terms: D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D007536:Isomerism; D008856:Microscopy, Fluorescence; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000494:pharmacology; D017395:Plasminogen Activator Inhibitor 1 / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D023303:Oxazolidinones; D017395:Plasminogen Activator Inhibitor 1