Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1

Ariamala Gopalsamy; Scott L Kincaid; John W Ellingboe; Thomas M Groeling; Thomas M Antrilli; Girija Krishnamurthy; Ann Aulabaugh; Gregory S Friedrichs; David L Crandall

doi:10.1016/j.bmcl.2004.04.058

Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3477-80. doi: 10.1016/j.bmcl.2004.04.058.

Authors

Ariamala Gopalsamy¹, Scott L Kincaid, John W Ellingboe, Thomas M Groeling, Thomas M Antrilli, Girija Krishnamurthy, Ann Aulabaugh, Gregory S Friedrichs, David L Crandall

Affiliation

¹ Chemical and Screening Sciences, Wyeth Research, 401 N Middletown Road, Pearl River, NY 10965, USA. [email protected]

PMID: 15177456
DOI: 10.1016/j.bmcl.2004.04.058

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.

MeSH terms

Drug Design
Humans
Inhibitory Concentration 50
Isomerism
Microscopy, Fluorescence
Oxazolidinones / chemical synthesis
Oxazolidinones / pharmacology
Plasminogen Activator Inhibitor 1 / metabolism*
Structure-Activity Relationship

Substances

Oxazolidinones
Plasminogen Activator Inhibitor 1