Synthesis and in Vitro Evaluation of a Series of Diketopiperazine Inhibitors of Plasminogen Activator Inhibitor-1

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2001 Sep 12

PMID 11551756

Citations 10

Authors

A Folkes

M B ROE

S Sohal

J Golec

R Faint

T Brooks

P Charlton

Affiliations

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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.

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