Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1

A Folkes; M B Roe; S Sohal; J Golec; R Faint; T Brooks; P Charlton

doi:10.1016/s0960-894x(01)00508-x

Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1

Bioorg Med Chem Lett. 2001 Oct 8;11(19):2589-92. doi: 10.1016/s0960-894x(01)00508-x.

Authors

A Folkes¹, M B Roe, S Sohal, J Golec, R Faint, T Brooks, P Charlton

Affiliation

¹ Xenova Limited, 957 Buckingham Avenue, Slough, Berks SL1 4NL, UK. [email protected]

PMID: 11551756
DOI: 10.1016/s0960-894x(01)00508-x

Abstract

We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC(50)=0.2 microM. The synthesis and SAR of these compounds are described.

MeSH terms

Diketopiperazines
Piperazines / chemical synthesis*
Piperazines / chemistry
Piperazines / pharmacology
Plasminogen Activator Inhibitor 1 / metabolism*
Structure-Activity Relationship

Substances

Diketopiperazines
Piperazines
Plasminogen Activator Inhibitor 1
XR 5118