Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1

We have synthesized and evaluated a series of tetramic acid-based and hydroxyquinolinone-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). These studies resulted in the identification of several compounds which showed excellent potency against PAI-1. The design, synthesis and SAR of the...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-04, Vol.12 (7), p.1063-1066
Main Authors: FOLKES, Adrian, BROWN, S. David, LEAHY, James W, MACH, Morrison, MATTHEWS, David, PRISBYLLA, Michael P, SANDERSON, Jason, SIMON, Reyna J, TESFAI, Zerom, VICKER, Nigel, WANG, Shouming, WEBB, Robert R, CANNE, Lynne E, CHARLTON, Peter, CHAN, Jocelyn, ENGELHARDT, Erin, EPSHTEYN, Sergey, FAINT, Richard, GOLEC, Julian, HANEL, Art, KEARNEY, Patrick
Format: Article
Language:English
Subjects:
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Chromogenic Compounds - chemistry
Drug Design
Drug Evaluation
Hydroxyquinolines - chemical synthesis
Hydroxyquinolines - chemistry
Hydroxyquinolines - pharmacology
In Vitro Techniques
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Plasminogen Activator Inhibitor 1 - chemical synthesis
Plasminogen Activator Inhibitor 1 - chemistry
Plasminogen Activator Inhibitor 1 - pharmacology
Pyrrolidinones - chemistry
Structure-Activity Relationship
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:We have synthesized and evaluated a series of tetramic acid-based and hydroxyquinolinone-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). These studies resulted in the identification of several compounds which showed excellent potency against PAI-1. The design, synthesis and SAR of these compounds are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/s0960-894x(02)00078-1