title: Synthesis and biological evaluation of piperazine-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).
abstract: Compound 2 was identified by high throughput screening as a novel PAI-1 inhibitor. Systematic optimization of the A, B, and C segments of 2 resulted in the identification of a more potent compound 39 with good oral bioavailability. The synthesis and SAR data are presented in this report.
authors.affiliation: Discovery Research, Berlex Biosciences, 2600 Hilltop Drive, PO Box 4099, Richmond, CA 94804-0099, USA. bin_ye@berlex.com
authors.forename: Bin
authors.initials: B
authors.lastname: Ye
authors.forename: Yuo-Ling
authors.initials: YL
authors.lastname: Chou
authors.forename: Rushad
authors.initials: R
authors.lastname: Karanjawala
authors.forename: Wheeseong
authors.initials: W
authors.lastname: Lee
authors.forename: Shou-Fu
authors.initials: SF
authors.lastname: Lu
authors.forename: Kenneth J
authors.initials: KJ
authors.lastname: Shaw
authors.forename: Steven
authors.initials: S
authors.lastname: Jones
authors.forename: Dao
authors.initials: D
authors.lastname: Lentz
authors.forename: Amy
authors.initials: A
authors.lastname: Liang
authors.forename: Jih-Lie
authors.initials: JL
authors.lastname: Tseng
authors.forename: Qingyu
authors.initials: Q
authors.lastname: Wu
authors.forename: Zuchun
authors.initials: Z
authors.lastname: Zhao
mesh_terms: D000818:Animals; D001780:Blood Coagulation Tests; D004353:Drug Evaluation, Preclinical; D005342:Fibrinolysis / Q000187:drug effects; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D017395:Plasminogen Activator Inhibitor 1 / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D010879:Piperazines; D017395:Plasminogen Activator Inhibitor 1