title: Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1).
abstract: Compound 1 was identified by high throughput screening as a novel PAI-1 inhibitor. Optimization of the B and C-segments of 1 resulted in a series of structurally simplified compounds with improved potency. The synthesis and SAR data of these compounds are presented here.
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: Shawn
authors.initials: S
authors.lastname: Bauer
authors.forename: Brad O
authors.initials: BO
authors.lastname: Buckman
authors.forename: Ameen
authors.initials: A
authors.lastname: Ghannam
authors.forename: Brian D
authors.initials: BD
authors.lastname: Griedel
authors.forename: Seock-Kyu
authors.initials: SK
authors.lastname: Khim
authors.forename: Wheeseong
authors.initials: W
authors.lastname: Lee
authors.forename: Karna L
authors.initials: KL
authors.lastname: Sacchi
authors.forename: Kenneth J
authors.initials: KJ
authors.lastname: Shaw
authors.forename: Amy
authors.initials: A
authors.lastname: Liang
authors.forename: Qingyu
authors.initials: Q
authors.lastname: Wu
authors.forename: Zuchun
authors.initials: Z
authors.lastname: Zhao
mesh_terms: D000818:Animals; D004353:Drug Evaluation, Preclinical / Q000379:methods; D000432:Methanol / Q000138:chemical synthesis* / Q000494:pharmacology*; D017395:Plasminogen Activator Inhibitor 1 / Q000378:metabolism*; D051381:Rats
chemical_list: D017395:Plasminogen Activator Inhibitor 1; D000432:Methanol